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| Gene | BRAF |
| Variant | V600E |
| Impact List | missense |
| Protein Effect | gain of function |
| Gene Variant Descriptions | BRAF V600E (previously reported as V599E) lies within the activation segment of the kinase domain of the Braf protein (PMID: 15035987). V600E confers a gain of function to the Braf protein as demonstrated by increased Braf kinase activity, downstream signaling, and the ability to transform cells in culture (PMID: 15035987, PMID: 29533785, PMID: 18697864). |
| Associated Drug Resistance | |
| Category Variants Paths |
BRAF mutant BRAF act mut BRAF V600E/K BRAF V600E BRAF mutant BRAF V600X BRAF V600E/K BRAF V600E |
| Transcript | NM_004333.6 |
| gDNA | chr7:g.140753336A>T |
| cDNA | c.1799T>A |
| Protein | p.V600E |
| Source Database | RefSeq |
| Genome Build | GRCh38/hg38 |
| Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
|---|---|---|---|---|---|
| NM_004333 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_001378474.1 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_004333.5 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_001354609.2 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| XM_005250045 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_001354609.1 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_001378468.1 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| NM_004333.6 | chr7:g.140753336A>T | c.1799T>A | p.V600E | RefSeq | GRCh38/hg38 |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E | thyroid cancer | predicted - sensitive | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mekinist (trametinib) inhibited growth of both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| BRAF V600E | melanoma | sensitive | Trametinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (METRIC) that supported FDA approval, Mekinist (trametinib) treatment, as compared to Deticine (dacarbazine) or Taxol (paclitaxel) treatment, resulted in improved progression-free survival of 4.8 months versus 1.5 months and an overall six month survival rate of 81% versus 67% in patients with BRAF V600E/K-positive metastatic melanoma (PMID: 22663011; NCT01245062). | 22663011 detail... detail... |
| BRAF V600E | lung adenocarcinoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, of 4 patients with lung adenocarcinoma, 1 achieved a partial response with an ongoing progression-free survival (PFS) at 32.5 mo, 3 patients had stable disease for 15.6, 6.6, and 3.6 mo, and an additional unevaluable patient achieved an 81% reduction of measured lesions and a PFS of 12.7 mo (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, 1 patient with pleomorphic xanthoastrocytoma achieved a partial response lasting 7.2 months (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | intrahepatic cholangiocarcinoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, of 4 patients with intrahepatic cholangiocarcinoma, 3 achieved a partial response, with individual progression-free survival of 12.8, 9.1, and 29.4 months (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | peritoneal serous papillary adenocarcinoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, 1 patient with mucinous-papillary serous adenocarcinoma of the peritoneum achieved a partial response (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | colorectal cancer | sensitive | Trametinib | Preclinical | Actionable | In a preclinical study, colorectal cancer cells harboring a BRAF V600E mutation had increased sensitivity to Mekinist (trametinib) compared to other colorectal cancer lines in culture (PMID: 25309914). | 25309914 |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, of 5 patients with low grade serous ovarian carcinoma, 4 achieved a partial response (PR), 1 had stable disease, 3 of the PRs lasted over 12 months (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | triple-receptor negative breast cancer | sensitive | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mekinist (trametinib) treatment inhibited Mapk signaling and viability in a triple-negative breast cancer cell line harboring BRAF V600E in culture (PMID: 36011019). | 36011019 |
| BRAF V600E | histiocytic sarcoma | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with advanced solid tumors harboring BRAF V600E, 1 patient with histiocytic sarcoma of the brain achieved a partial response with an ongoing progression-free survival at 20.9 months (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | diffuse leptomeningeal glioneuronal tumor | predicted - sensitive | Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) treatment resulted in a partial response in the brain and stable disease in the spine in a pediatric patient with diffuse leptomeningeal glioneuronal tumor harboring BRAF V600E (PMID: 39399174). | 39399174 |
| BRAF V600E | Advanced Solid Tumor | predicted - sensitive | Trametinib | Phase II | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment resulted in an objective response rate of 37.9% (11/29) in patients with BRAF V600E positive advanced solid tumors other than melanoma, thyroid cancer, or colorectal cancer, with a median duration of response of 25.1 months, and a disease control rate of 75.9% (22/29) (PMID: 32758030; NCT02465060). | 32758030 |
| BRAF V600E | melanoma | sensitive | Dabrafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III clinical trial (BREAK-3) that supported FDA approval, Tafinlar (dabrafenib) improved median progression-free survival compared to Deticene (dacarbazine) (5.1 vs 2.7 months, HR=0.3, p<0.0001) in patients with BRAF V600E positive melanoma (PMID: 22735384; NCT01227889). | detail... detail... 22735384 |
| BRAF V600E | nephroblastoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a durable major response with a decrease in the pulmonary metastases in an adult patient with metastatic nephroblastoma harboring BRAF V600E (PMID: 31109800). | 31109800 |
| BRAF V600E | glioblastoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, a previously treated pediatric patient with epithelioid glioblastoma harboring BRAF V600E demonstrated stable disease for 10 months when treated with Tafinlar (dabrafenib) (PMID: 29621181). | 29621181 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Dabrafenib | Phase II | Actionable | In a Phase II trial, 33% (26/78) of previously treated non-small cell lung carcinoma patients harboring BRAF V600E demonstrated an overall response, which included all partial responses, when treated with Tafinlar (dabrafenib) while 67% (4/6) receiving Tafinlar (dabrafenib) as a first-line treatment achieved partial responses (PMID: 27080216; NCT01336634). | 27080216 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Dabrafenib | Guideline | Actionable | Tafinlar (dabrafenib) is in guidelines as a first-line therapy for patients with advanced or metastatic non-small cell lung cancer with BRAF V600E mutations who can not tolerate the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) (NCCN.org). | detail... |
| BRAF V600E | follicular thyroid carcinoma | sensitive | Dabrafenib | Guideline | Actionable | Tafinlar (dabrafenib) is included in guidelines for patients with recurrent, advanced, or metastatic thyroid follicular carcinoma harboring BRAF V600E for whom clinical trials are not available or appropriate (NCCN.org). | detail... |
| BRAF V600E | thyroid gland carcinoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Tafinlar (dabrafenib) treatment resulted in a partial response in 29% (4/14) and stable disease in 43% (6/14) of patients with thyroid carcinoma harboring BRAF V600E, with 64% (9/14) of patients achieved at least a 10% decrease by RECIST, and a median progression-free survival of 11.3 months among responders (PMID: 25285888; NCT00880321). | 25285888 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Dabrafenib | Clinical Study - Cohort | Actionable | In a clinical study, Tafinlar (dabrafenib) treatment stimulated radioiodine uptake in 60% (6/10) of patients with metastatic iodine-refractory papillary thyroid cancer harboring BRAF V600E (PMID: 25549723; NCT01534897). | 25549723 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Dabrafenib | Guideline | Actionable | Tafinlar (dabrafenib) is included in guidelines for patients with recurrent, advanced, or metastatic thyroid papillary carcinoma harboring BRAF V600E for whom clinical trials are not available or appropriate (NCCN.org). | detail... |
| BRAF V600E | colon neuroendocrine neoplasm | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment of a patient with recurrent neuroendocrine carcinoma of the colon harboring a BRAF V600E mutation resulted in stable disease for 6 months before disease progression (PMID: 30181415). | 30181415 |
| BRAF V600E | Erdheim-Chester disease | sensitive | Dabrafenib | Guideline | Actionable | Tafinlar (dabrafenib) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | pilocytic astrocytoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a near complete response and resolution of leptomeningeal dissemination in a patient with pilocytic astrocytoma harboring BRAF V600E (PMID: 28784858). | 28784858 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in 1 partial response and 1 stable disease in 2 patients with tempero-parietal pleomorphic xanthoastrocytoma harboring BRAF V600E and CDKN2A deletion (PMID: 39399174). | 39399174 |
| BRAF V600E | ganglioglioma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a partial response in two pediatric patients with ganglioglioma (1 suprasellar ganglioglioma, 1 cervicomedullary ganglioglioma) harboring BRAF V600E (PMID: 39399174). | 39399174 |
| BRAF V600E | ganglioglioma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in partial response 8 weeks after therapy initiation in a pediatric patient with anaplastic ganglioglioma harboring BRAF V600E, but disease progression occurred at 40 weeks due to acquired resistance (PMID: 29880583). | 29880583 |
| BRAF V600E | ganglioglioma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical study, Tafinlar (dabrafenib) treatment resulted in symptomatic improvement and clinical efficacy in three pediatric patients with brainstem ganglioglioma harboring BRAF V600E, with decreased tumor volume and treatment continuing for at least 5.5 years in one patient, a significant partial response in another patient, and a partial response in a third patient with tumor regression and ongoing response for at least 2 years (PMID: 31502039). | 31502039 |
| BRAF V600E | skin melanoma | sensitive | Dabrafenib | Guideline | Actionable | Tafinlar (dabrafenib) therapy is included in guidelines for cutaneous melanoma patients with unresectable or metastatic disease harboring BRAF V600 activating mutations, such as BRAF V600E, in cases where BRAF/MEK inhibitor combination therapy is contraindicated (NCCN.org). | detail... |
| BRAF V600E | gastrointestinal stromal tumor | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a 20% decrease in tumor size after 24 weeks in a patient with a gastrointestinal stromal tumor harboring BRAF V600E (PMID: 23470635). | 23470635 |
| BRAF V600E | gastrointestinal stromal tumor | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, third-line treatment with Tafinlar (dabrafenib) resulted in a partial response lasting 19 months in a patient with gastrointestinal stromal tumor harboring BRAF V600E (PMID: 38756640). | 38756640 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib | Preclinical | Actionable | In a preclinical study, colorectal cancer cell lines harboring a BRAF V600E mutation had increased sensitivity to Tafinlar (dabrafenib) in culture compared to cell lines with wild-type BRAF (PMID: 24885690). | 24885690 |
| BRAF V600E | triple-receptor negative breast cancer | sensitive | Dabrafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Tafinlar (dabrafenib) treatment inhibited Mapk signaling and viability in a triple-negative breast cancer cell line harboring BRAF V600E in culture (PMID: 36011019). | 36011019 |
| BRAF V600E | anaplastic pleomorphic xanthoastrocytoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a partial response in a patient with tempero-parietal anaplastic pleomorphic xanthoastrocytoma harboring BRAF V600E (PMID: 39399174). | 39399174 |
| BRAF V600E | desmoplastic infantile ganglioglioma / desmoplastic infantile astrocytoma | predicted - sensitive | Dabrafenib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) treatment resulted in a partial response with resolution of ascites in a pediatric patient with suprasellar metastatic desmoplastic infantile astrocytoma harboring BRAF V600E (PMID: 39399174). | 39399174 |
| BRAF V600E | hairy cell leukemia | sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in complete resolution of the brain lesions after 3 months of treatment, decreased spleen size, and resolution of leukemic retinopathy in a patient with hairy cell leukemia harboring BRAF V600E (PMID: 36713531). | 36713531 |
| BRAF V600E | hairy cell leukemia | sensitive | Vemurafenib | Phase II | Actionable | In two Phase II clinical studies, patients with refractory hairy cell leukemia harboring BRAF V600E responded to Zelboraf (vemurafenib) with overall response rates of 96% (25/26) and 100% (24/24) as well as complete response rates of 35% (9/26) and 42% (10/24) with median follow up times of 8 and 12 weeks, respectively (PMID: 26352686). | 26352686 |
| BRAF V600E | sarcoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in sarcoma patients harboring BRAF V600E (n=6) when treated with Zelboraf (vemurafenib), including 1 patient with a complete response and 1 patient with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | thyroid cancer | conflicting | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in complete response in a patient with anaplastic thyroid cancer harboring BRAF V600E (PMID: 29320312; NCT02091141). | 29320312 |
| BRAF V600E | thyroid cancer | conflicting | Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, thyroid cancer cells harboring BRAF V600E demonstrated decreased sensitivity to Zelboraf (vemurafenib) in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | pancreatic endocrine carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with pancreatic endocrine carcinoma found to harbor BRAF V600E demonstrated stable disease and some tumor shrinkage when treated with Zelboraf (vemurafenib) (PMID: 31158244). | 31158244 |
| BRAF V600E | neuroendocrine carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in patients with neuroendocrine carcinoma harboring BRAF V600E (n=3) when treated with Zelboraf (vemurafenib), including 1 patient with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | melanoma | sensitive | Vemurafenib | Phase I | Actionable | In a Phase I trial, Zelboraf (vemurafenib) treatment resulted in an overall response rate of 81% (26/32; 2 complete responses, 24 partial responses), and inhibition of tumor Erk and Ccnd1, and reduced cell proliferation in metastatic melanoma patients harboring BRAF V600E (PMID: 20818844; NCT00215605). | 20818844 |
| BRAF V600E | melanoma | sensitive | Vemurafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (BRIM-3) that supported FDA approval, Zelboraf (vemurafenib), as compared to Deticene (dacarbazine), resulted in an improved overall survival (OS) (13.6 vs 9.7 months, HR=0.81, p=0.03) in patients with BRAF V600E-positive metastatic melanoma, with estimated OS rates of 56%, 30%, 21%, and 17% at 1, 2, 3, and 4 years, respectively (PMID: 28961848, PMID: 21639808; NCT01006980), and BRAF V600E is included on the companion diagnostic (FDA.gov). | 28961848 detail... detail... 21639808 |
| BRAF V600E | ovarian cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in an objective response of 50% (2/4, 2 partial response) in patients with ovarian cancer harboring BRAF V600E, and stable disease lasting more than 120 days in 1 patient (PMID: 29320312; NCT02091141). | 29320312 |
| BRAF V600E | ovarian cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in ovarian cancer patients harboring BRAF V600E (n=4) when treated with Zelboraf (vemurafenib), including 2 patients with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | larynx cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in complete response in a patient with larynx cancer harboring BRAF V600E (PMID: 29320312; NCT02091141). | 29320312 |
| BRAF V600E | glioblastoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a partial response 1 week after treatment in a patient with epithelioid type glioblastoma harboring BRAF V600E, although the patient soon passed due to complications (PMID: 31386052). | 31386052 |
| BRAF V600E | glioblastoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in tumor regression as confirmed by MRI after 3-weeks of treatment in a patient with epithelioid glioblastoma harboring BRAF V600E (PMID: 31217909). | 31217909 |
| BRAF V600E | glioblastoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in stable disease as best response in 3 of 6 patients with glioblastoma harboring BRAF V600E, with stable disease lasting 3.6, 3.7, and 12.9 months, respectively (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | high grade glioma | sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in glioma patients harboring BRAF V600E (n=24) when treated with Zelboraf (vemurafenib), including 1 patient with a complete response and 5 patients with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | high grade glioma | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in an objective response rate of 25% (6/24, 1 complete response, 5 partial responses) in patients with gliomas harboring BRAF V600E, with a median progression free survival of 5.5-months, a median overall survival of 28.2 months (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | high grade glioma | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines as adjuvant therapy for pediatric patients with diffuse high-grade gliomas harboring BRAF V600E, or as a preferred regimen for patients with recurrent or progressive disease (NCCN.org). | detail... |
| BRAF V600E | anaplastic astrocytoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in a partial response in 1 of 5 patients with anaplastic astrrocytoma harboring BRAF V600E, with 2 other patients achieved stable disease lasting 14.9, and 5.6 months, respectively (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | histiocytosis | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical study, Zelboraf (vemurafenib) treatment resulted in complete remission in 2 pediatric patients with Langerhans cell histiocytosis harboring BRAF V600E (PMID: 39190425). | 39190425 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, a non-small cell lung cancer patient harboring a BRAF V600E mutation had a complete response after treatment with Zelboraf (vemurafenib) (PMID: 23733758). | 23733758 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in an objective response of 43% (6/14, 1 complete response, 5 partial response) in patients with non-small cell lung cancer harboring BRAF V600E, and stable disease lasting more than 120 days in 2 patients (PMID: 29320312; NCT02091141). | 29320312 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial (VE-BASKET), responses were seen in patients with non-small cell lung cancer harboring BRAF V600E (n=63) when treated with Zelboraf (vemurafenib), including 23 patients with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Vemurafenib | Clinical Study | Actionable | In a retrospective analysis, non-small cell lung cancer patients harboring BRAF V600E achieved an overall response rate of 54% (13/24, 2 complete responses, 11 partial responses, and 10 with stable disease) and a disease control rate of 96% following treatment with Zelboraf (vemurafenib) (PMID: 26200454). | 26200454 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines as a first-line therapy for advanced or metastatic non-small cell lung cancer patients harboring BRAF V600E mutations who can not tolerate the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) (NCCN.org). | detail... |
| BRAF V600E | follicular thyroid carcinoma | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines for patients with recurrent, advanced, or metastatic thyroid follicular carcinoma harboring BRAF V600E for whom clinical trials are not available or appropriate (NCCN.org). | detail... |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a partial response with approximately 90% tumor shrinkage and a progression-free survival of 10 months in a patient with metastatic papillary thyroid carcinoma harboring BRAF V600E (PMID: 38489728). | 38489728 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Zelboraf (vemurafenib) treatment resulted in a complete or partial response in three papillary thyroid carcinoma patients harboring BRAF V600E, with one patient having a response that lasted for 8 months who remained progression-free for 12 months, and another two patients having a stable disease that lasted for 11 and 13 months, respectively (PMID: 20818844; NCT00215605). | 20818844 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial, Zelboraf (vemurafenib) treatment resulted in a partial response in 38.5% (10/26) of patients with metastatic or unresectable, radioactive iodine-refractory papillary thyroid carcinoma harboring BRAF V600E that were multikinase inhibitor-naive, with a disease control rate of 73%, and a median progression-free survival of 18.2 months (PMID: 27460442; NCT01286753). | 27460442 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines for patients with recurrent, advanced, or metastatic thyroid papillary carcinoma harboring BRAF V600E for whom clinical trials are not available or appropriate (NCCN.org). | detail... |
| BRAF V600E | Erdheim-Chester disease | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines as preferred first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | renal cell carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic renal cell carcinoma harboring BRAF V600E demonstrated a partial response following treatment with Zelboraf (vemurafenib) (PMID: 26918217). | 26918217 |
| BRAF V600E | pilocytic astrocytoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in a partial response in a patient with pilocytic astrrocytoma harboring BRAF V600E who stayed on treatment for 15.3 months (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a complete intracranial response 2 months after treatment in a patient with anaplastic pleomorphic xanthoastrocytoma harboring BRAF V600E, although the disease progressed 1 month later (PMID: 31386052). | 31386052 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in an objective response rate of 42.9% (3/7, 1 complete response, 2 partial responses) and a clinical benefit rate of 57% in patients with pleomorphic xanthoastrocytoma harboring BRAF V600E, with a median progression-free survival of 5.7 months, and median overall survival not reached (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | cholangiocarcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in patients with cholangiocarcinoma harboring BRAF V600E (n=9) when treated with Zelboraf (vemurafenib), including 2 patients with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | ganglioglioma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in a partial response in a patient with anaplastic ganglioglioma harboring BRAF V600E who stayed on treatment for 13.8 months (PMID: 30351999; NCT01524978). | 30351999 |
| BRAF V600E | synovial sarcoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) resulted in a partial response after 4 months of treatment in a patient with intrathoracic synovial sarcoma harboring SS18-SSX1 (e10:e6) and BRAF V600E (PMID: 37417899). | 37417899 |
| BRAF V600E | histiocytic and dendritic cell cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), responses were seen in patients with histiocytic neoplasms harboring BRAF V600E (n=27) when treated with Zelboraf (vemurafenib), including 15 patients with a partial response and 2 patients with a complete response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | ovary serous adenocarcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a partial response lasting more than 21 months in a patient with low grade serous ovarian adenocarcinoma harboring BRAF V600E (PMID: 26490654). | 26490654 |
| BRAF V600E | ovarian serous cystadenocarcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a complete radiological response that lasted for 3 years in a patient with low-grade serous cystadenocarcinoma of the ovary harboring BRAF V600E (PMID: 36967525). | 36967525 |
| BRAF V600E | childhood pilocytic astrocytoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a partial response in a pediatric patient with pilocytic astrocytoma harboring BRAF V600E (PMID: 38976815). | 38976815 |
| BRAF V600E | oncocytic carcinoma of the thyroid | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) is included in guidelines for patients with recurrent, advanced, or metastatic thyroid Hurthle cell carcinoma harboring BRAF V600E for whom clinical trials are not available or appropriate (NCCN.org). | detail... |
| BRAF V600E | salivary gland cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), a patient with salivary ductal carcinoma harboring BRAF V600E demonstrated a partial response when treated with Zelboraf (vemurafenib) (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | skin melanoma | sensitive | Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) therapy is included in guidelines for cutaneous melanoma patients with unresectable or metastatic disease harboring BRAF V600 activating mutations, such as BRAF V600E, in cases where BRAF/MEK inhibitor combination therapy is contraindicated (NCCN.org). | detail... |
| BRAF V600E | colorectal cancer | no benefit | Vemurafenib | Phase II | Actionable | In a Phase II trial, Zelboraf (vemurafenib) did not demonstrate meaningful clinical activity as a single agent, resulted in partial response in 5% (1/21) and stable disease in 33% (7/21) of patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 26460303; NCT00405587). | 26460303 |
| BRAF V600E | colorectal cancer | no benefit | Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cancer cell lines harboring BRAF V600E demonstrated decreased response to Zelboraf (vemurafenib) in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | no benefit | Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, colorectal cancer cell lines harboring BRAF V600E were not sensitive to growth inhibition by Zelboraf (vemurafenib) in culture or xenograft models, due to feedback activation of EGFR signaling (PMID: 22281684). | 22281684 |
| BRAF V600E | ameloblastoma | sensitive | Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Zelboraf (vemurafenib) inhibited viability of ameloblastoma cell lines harboring BRAF V600E in culture (PMID: 35689405). | 35689405 |
| BRAF V600E | ameloblastoma | sensitive | Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Zelboraf (vemurafenib) inhibited viability of an ameloblastoma cell line harboring BRAF V600E in culture (PMID: 24859340). | 24859340 |
| BRAF V600E | salivary gland carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II (MyPathway) trial, Zelboraf (vemurafenib) treatment resulted in a partial response in a patient with advanced salivary gland carcinoma harboring BRAF V600E, with a progression-free survival of 18.5 months (PMID: 32067683; NCT02091141). | 32067683 |
| BRAF V600E | triple-receptor negative breast cancer | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in a partial response in the lung lesion lasting at least 19 months in a patient with metastatic triple-negative breast cancer harboring BRAF V600E (PMID: 33976643). | 33976643 |
| BRAF V600E | anaplastic thyroid carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, first-line adjuvant therapy with Zelboraf (vemurafenib) resulted in a partial remission of the tumor and lymphatic and pulmonary metastases after 36 days of treatment in a patient with analplastic thyroid carcinoma harboring BRAF V600E, with a near-complete regression observed within 5 months of treatment initiation (PMID: 36855200). | 36855200 |
| BRAF V600E | anaplastic thyroid carcinoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in a response in patients with anaplastic thyroid carcinoma harboring BRAF V600E (n=12), including 1 patient with a complete response and 2 patients with a partial response (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | IDH-wildtype glioblastoma | predicted - sensitive | Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) treatment resulted in disease stability over 15 months in a patient with epithelioid glioblastoma harboring BRAF V600E, who previously progressed on conventional treatment options (PMID: 34232949). | 34232949 |
| BRAF V600E | Advanced Solid Tumor | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in an objective response of 46% (12/26, 2 complete response, 10 partial response) in patients with advanced solid tumors harboring BRAF V600E, but only 4% (1/23, 1 partial response) in patients harboring non-V600 BRAF mutations (PMID: 29320312; NCT02091141). | 29320312 |
| BRAF V600E | Advanced Solid Tumor | sensitive | Vemurafenib | Phase II | Actionable | In a Phase II trial (VE-BASKET), Zelboraf (vemurafenib) treatment resulted in an objective response rate of 33% (56/172) in patients with advanced solid tumors harboring BRAF V600E, including 5 patients with a complete response and 51 patients with a partial response, and led a duration of response of 13.1 months, a progression-free survival of 5.8 months, and an overall survival of 17.6 months (PMID: 32029534; NCT01524978). | 32029534 |
| BRAF V600E | glioblastoma | sensitive | BI2536 | Preclinical - Cell culture | Actionable | In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated sensitivity to BI2536 in culture (PMID: 26573800). | 26573800 |
| BRAF V600E | colon cancer | resistant | Cetuximab | Guideline | Actionable | Erbitux (cetuximab), as a monotherapy, is not indicated for use in colon cancer patients with BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | rectum cancer | resistant | Cetuximab | Guideline | Actionable | Erbitux (cetuximab), as a monotherapy, is not indicated for use in rectum cancer patients with BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | colorectal cancer | resistant | Cetuximab | Guideline | Actionable | Erbitux (cetuximab), as a monotherapy, is not indicated for use in metastatic colorectal cancer patients with BRAF V600E (PMID: 36307056; ESMO.org). | 36307056 detail... |
| BRAF V600E | ovarian cancer | sensitive | CI-1040 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CI-1040 inhibited growth of a human ovarian cancer cell line harboring BRAF V600E in culture, and inhibited tumor growth in xenograft models (PMID: 19018267). | 19018267 |
| BRAF V600E | Advanced Solid Tumor | sensitive | CI-1040 | Preclinical | Actionable | In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation and growth of transformed cells expressing BRAF V600E in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | melanoma | sensitive | Dasatinib | Preclinical | Actionable | In a preclinical study, Sprycel (dasatinib) inhibited cell invasion, cell signaling, and proliferation in human melanoma cell lines harboring BRAF V600E that are resistant to Braf inhibition in culture and in animal models (PMID: 23242808). | 23242808 |
| BRAF V600E | lung carcinoma | resistant | Dasatinib | Preclinical | Actionable | In a preclinical study, Sprycel (dasatinib) failed to induce apoptosis in lung carcinoma cells expressing BRAF V600E (PMID: 22649091). | 22649091 |
| BRAF V600E | skin melanoma | sensitive | Ganetespib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the Hsp90 inhibitor Ganetespib destabilized BRAF, especially BRAF V600E, resulted in loss of cell viability in culture and antitumor effects in cell line xenograft models of melanoma (PMID: 24398428). | 24398428 |
| BRAF V600E | melanoma | sensitive | GSK2126458 | Preclinical | Actionable | In a preclinical study, Omipalisib (GSK2126458) inhibited the growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 22389471). | 22389471 |
| BRAF V600E | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) treatment inhibited Erk phosphorylation and reduced proliferation of melanoma cells harboring monomeric BRAF V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | melanoma | sensitive | Encorafenib | Preclinical - Cell line xenograft | Actionable | In preclinical studies, Encorafenib (LGX818) treatment of human melanoma xenograft models with BRAF V600E significantly decreased Mek activation and resulted in tumor regression (Cancer Res: 72(8) Suppl 1, Abstract #3790). | detail... |
| BRAF V600E | pseudomyxoma peritonei | sensitive | Encorafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability and induced apoptosis in a patient-derived pseudomyxoma peritonei cell line harboring BRAF V600E in culture and inhibited tumor growth and improved survival of a patient-derived xenograft (PDX) model (PMID: 39018564). | 39018564 |
| BRAF V600E | colorectal cancer | sensitive | Encorafenib | Phase I | Actionable | In a Phase I trial, Encorafenib (LGX818) showed activity in patients with advanced metastatic colorectal cancer harboring a BRAF V600E mutation, resulting in a median progression-free survival of 4 months and a best response of stable disease in 66.7% (12/18) (Ann Oncol (2014) 25 (suppl 4): iv182-iv183). | detail... |
| BRAF V600E | melanoma | predicted - sensitive | Abemaciclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Verzenio (abemaciclib) induced apoptosis in Zelboraf (vemurafenib)-resistant melanoma cells harboring BRAF V600E in culture, and induced tumor regression in xenograft models (PMID: 25122067). | 25122067 |
| BRAF V600E | colon neuroendocrine neoplasm | no benefit | Binimetinib | Case Reports/Case Series | Actionable | In Phase II trial, Mektovi (binimetinib) therapy in a patient with recurrent neuroendocrine carcinoma of the colon harboring a BRAF V600E mutation who had previously progressed on Tafinlar (dabrafenib) resulted in disease progression after two cycles (PMID: 30181415; NCT01885195). | 30181415 |
| BRAF V600E | triple-receptor negative breast cancer | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) treatment inhibited Mapk signaling and viability in a triple-negative breast cancer cell line harboring BRAF V600E in culture (PMID: 36011019). | 36011019 |
| BRAF V600E | colon cancer | resistant | Panitumumab | Guideline | Actionable | Vectibix (panitumumab), as a monotherapy, is not indicated for use in colon cancer patients with BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | rectum cancer | resistant | Panitumumab | Guideline | Actionable | Vectibix (panitumumab), as a monotherapy, is not indicated for use in rectum cancer patients with BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | colorectal cancer | resistant | Panitumumab | Guideline | Actionable | Vectibix (panitumumab), as a monotherapy, is not indicated for use in metastatic colorectal cancer patients with BRAF V600E (PMID: 36307056; ESMO.org). | 36307056 detail... |
| BRAF V600E | colon cancer | sensitive | PD-0325901 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PD-0325901 demonstrated antitumor activity against BRAF V600E colon cancer cell line xenografts (PMID: 16273091). | 16273091 |
| BRAF V600E | melanoma | conflicting | PD-0325901 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma cell line xenograft model harboring BRAF V600E treated with PD-0325901 demonstrated stable tumor growth, but by day 44, growth ensued and thus, demonstrated no benefit (PMID: 27488531). | 27488531 |
| BRAF V600E | melanoma | conflicting | PD-0325901 | Preclinical - Cell culture | Actionable | In a preclinical study, PD-0325901 inhibited growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| BRAF V600E | melanoma | conflicting | PD-0325901 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PD-0325901 treatment induced cell cycle arrest and inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 25422890). | 25422890 |
| BRAF V600E | glioblastoma | conflicting | PD-0325901 | Preclinical - Cell culture | Actionable | In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated a decreased response to treatment with PD-0325901, demonstrating increased viability of CD133 positive cells in culture (PMID: 26573800). | 26573800 |
| BRAF V600E | glioblastoma | conflicting | PD-0325901 | Preclinical - Cell culture | Actionable | In a preclinical study, PD-0325901 inhibited growth of glioblastoma cell lines harboring BRAF V600E in culture (PMID: 38714355). | 38714355 |
| BRAF V600E | colorectal cancer | sensitive | PD-0325901 | Preclinical | Actionable | In a preclinical study, PD-0325901 inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| BRAF V600E | melanoma | no benefit | Palbociclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with Ibrance (palbociclib) in a melanoma cell line xenograft model harboring BRAF V600E resulted in no benefit, demonstrating low but continuous growth (PMID: 27488531). | 27488531 |
| BRAF V600E | colorectal cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 23629727). | 23629727 |
| BRAF V600E | melanoma | predicted - sensitive | RAF265 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with RAF265 in melanoma patients resulted in an objective response rate of 12.1% (8/66), including a partial response in four patients harboring BRAF V600E, two partial responses and one complete response in patients with wild-type BRAF, and one complete response in a patient with unknown mutational status (PMID: 28719152). | 28719152 |
| BRAF V600E | Advanced Solid Tumor | sensitive | RAF265 | Preclinical | Actionable | In a preclinical study, RAF265 inhibited Erk phosphorylation and cell proliferation in BRAF V600E expressing cells in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | melanoma | sensitive | Refametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Refametinib (BAY86-9766) inhibited growth of melanoma cell lines harboring BRAF V600E in culture and suppressed tumor growth in cell line xenograft models (PMID: 19706763). | 19706763 |
| BRAF V600E | colorectal cancer | sensitive | Refametinib | Preclinical | Actionable | In a preclinical study, Refametinib (BAY86-9766) inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture and suppressed tumor growth in cell line xenograft models (PMID: 19706763). | 19706763 |
| BRAF V600E | colorectal cancer | sensitive | Regorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture and suppressed angiogenesis and tumor growth in cell line xenograft models (PMID: 21170960). | 21170960 |
| BRAF V600E | melanoma | sensitive | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, RO4987655 inhibited proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 26438159). | 26438159 |
| BRAF V600E | melanoma | sensitive | Saracatinib | Preclinical | Actionable | In a preclinical study, saracatinib inhibited proliferation of human melanoma cell lines harboring BRAF V600E that are resistant to Braf inhibition in culture (PMID: 23242808). | 23242808 |
| BRAF V600E | thyroid cancer | sensitive | Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) inhibited growth of both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| BRAF V600E | melanoma | sensitive | Selumetinib | Phase II | Actionable | In a Phase II trial, a favorable response rate to selumetinib (AZD6244) was observed in mutant BRAF but not BRAF wild-type melanoma patients (PMID: 22048237). | 22048237 |
| BRAF V600E | pilocytic astrocytoma | sensitive | Selumetinib | Guideline | Actionable | Koselugo (selumetinib) is included in guidelines for patients with recurrent or progressive pilocytic astrocytoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | childhood pilocytic astrocytoma | predicted - sensitive | Selumetinib | Phase I | Actionable | In a Phase I trial, Koselugo (selumetinib) treatment resulted in a sustained partial response (PR) in 36% (9/25) and stable disease in 36% (9/25) of pediatric patients with pilocytic astrocytoma harboring KIAA1549-BRAF (n=18) or BRAF V600E (n=7), with a 2-year progression-free survival of 70%, and 29% (2/7) of the patients harboring BRAF V600E achieved PR (PMID: 31151904; NCT01089101). | 31151904 |
| BRAF V600E | colorectal cancer | sensitive | Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) decreased tumor growth in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 23942066). | 23942066 |
| BRAF V600E | Advanced Solid Tumor | no benefit | Selumetinib | Case Reports/Case Series | Actionable | In a Phase II trial (Pediatric MATCH), Koselugo (selumetinib) treatment was tolerated but did not result in an objective response in pediatric patients with advanced solid tumors including high-grade glioma (n=8) and rhabdomyosarcoma (n=7) harboring MAPK pathway alterations including BRAF V600E (n=2), activating KRAS (n=8)/HRAS (n=1)/NRAS (n=3) or inactivating NF1 (n=7) mutations, with a 6-month progression-free survival of 15% (3/20) and 3 stable disease as best response (PMID: 35363510; NCT03213691). | 35363510 |
| BRAF V600E | melanoma | no benefit | Sorafenib | Phase II | Actionable | In a Phase II study, Nexavar (sorafenib) displayed negligible efficacy in melanoma patients with BRAF V600E mutations (PMID: 16880785, PMID: 22394203). | 22394203 16880785 |
| BRAF V600E | colorectal cancer | sensitive | Sorafenib | Preclinical | Actionable | In a preclinical study, colorectal cancer cell lines harboring a BRAF V600E mutation were sensitive to Nexavar (sorafenib) in culture (PMID: 24885690). | 24885690 |
| BRAF V600E | lung cancer | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in two patients with lung cancer each harboring BRAF V600E (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF V600E | melanoma | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited Erk signaling in melanoma cells harboring BRAF V600E, resulted in cell cycle arrest in culture and tumor growth inhibition in cell line xenograft models (PMID: 28939558). | 28939558 |
| BRAF V600E | glioblastoma | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in a patient with glioblastoma harboring BRAF V600E (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF V600E | glioblastoma | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In an expanded access program (ULI-EAP-100), Ulixertinib (BVD-523) treatment resulted in clinical benefit in a patient with glioblastoma harboring BRAF V600E who stayed on treatment for 128 days (J Clin Oncol 40, no. 16_suppl (June 01, 2022) e15101; NCT04566393). | detail... |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In an expanded access program (ULI-EAP-100), Ulixertinib (BVD-523) treatment resulted in clinical benefit in a patient with pancreatic ductal adenocarcinoma harboring BRAF V600E who stayed on treatment for 413 days (J Clin Oncol 40, no. 16_suppl (June 01, 2022) e15101; NCT04566393). | detail... |
| BRAF V600E | central nervous system cancer | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase II trial (APEC1621J), Ulixertinib (BVD-523) treatment resulted in a 6-month progression-free survival rate of 37% but no objective response in pediatric and young adult patients with advanced solid tumors harboring MAPK pathway activation, however, a patient with glioneuronal tumor harboring a BRAF V600E achieved prolonged stable disease and remained on treatment for 9 cycles (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3009; NCT03698994). | detail... |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) reduced metabolic activity and inhibited MAPK pathway activity in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture, and inhibited tumor growth and improved survival compared to vehicle (48.5 days vs 30 days, respectively) in a xenograft model (PMID: 35882450). | 35882450 |
| BRAF V600E | colorectal cancer | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited Erk signaling in colorectal cancer cells harboring BRAF V600E, resulted in cell cycle arrest in culture and tumor growth inhibition in cell line xenograft models (PMID: 28939558). | 28939558 |
| BRAF V600E | colon carcinoma | sensitive | RXDX-105 | Preclinical - Cell line xenograft | Actionable | In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human colon carcinoma cell line (PMID: 22319199). | 22319199 |
| BRAF V600E | melanoma | sensitive | RXDX-105 | Preclinical - Cell line xenograft | Actionable | In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human melanoma cell line (PMID: 22319199). | 22319199 |
| BRAF V600E | melanoma | predicted - sensitive | Cobimetinib | Case Reports/Case Series | Actionable | In a Phase I trial, Cotellic (cobimetinib) treatment resulted in a confirmed partial response in six melanoma patients harboring BRAF V600E (PMID: 27424159). | 27424159 |
| BRAF V600E | lymphatic system cancer | predicted - sensitive | Cobimetinib | Case Reports/Case Series | Actionable | In a Phase II trial, treatment with Cotellic (cobimetinib) in patients with histiocytic neoplasms resulted in a PET overall response rate of 89% (16/18), with complete response in 72% (13/18) and partial response in 17% (3/18), and resulted in stable disease in 6% (1/18) of patients, including 1 partial response and 3 complete responses in 4 patients with Erdheim-Chester disease harboring BRAF V600E (PMID: 30867592; NCT01953926). | 30867592 |
| BRAF V600E | melanoma | sensitive | E6201 | Case Reports/Case Series | Actionable | In a Phase I trial, a patient with metastatic melanoma and brain metastasis harboring BRAF V600E demonstrated an ongoing near complete response with an overall survival of more than 8 years, and preclinical analysis of melanoma cell lines harboring homozygous or heterozygous BRAF V600E in culture were sensitive to treatment with E6201 (PMID: 30264293). | 30264293 |
| BRAF V600E | melanoma | sensitive | E6201 | Preclinical | Actionable | In a preclinical study, E6201 inhibited Mapk pathway activation and proliferation of melanoma cell lines harboring BRAF V600E mutation in culture (PMID: 24448821). | 24448821 |
| BRAF V600E | melanoma | sensitive | Tovorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Ojemda (tovorafenib) treatment inhibited viability of a melanoma cell line harboring BRAF V600E in culture (PMID: 31618628). | 31618628 |
| BRAF V600E | colon cancer | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, Gedatolisib (PKI-587) inhibited Braf V600E in vitro and inhibited growth of human colon cancer cells harboring BRAF V600E in culture (PMID: 21325073, PMID: 24042735). | 24042735 21325073 |
| BRAF V600E | melanoma | sensitive | PLX8394 | Preclinical - Cell culture | Actionable | In a preclinical study, PLX8394 treatment inhibited Erk phosphorylation and reduced proliferation of melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | glioblastoma | predicted - sensitive | PLX8394 | Case Reports/Case Series | Actionable | In a clinical case study, PLX8394 treatment resulted in a radiographic partial response and complete resolution of symptoms for 7 months in a patient with glioblastoma harboring BRAF V600E, CDKN2A/B loss and CHEK2 T367fs were also identified in the tumor (PMID: 32923904; NCT02428712). | 32923904 |
| BRAF V600E | Advanced Solid Tumor | sensitive | PLX8394 | Preclinical | Actionable | In a preclinical study, PLX8394 had been shown to block survival and growth of vemurafenib/PLX4720-resistant cells harboring distinct BRAF V600E splice variants (PMID: 24422853). | 24422853 |
| BRAF V600E | melanoma | sensitive | BI-847325 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with BI-847325 resulted in decreased expression of Mcl-1 and Mek, and inhibited growth of melanoma cell lines harboring BRAF V600E in culture, and inhibited tumor growth in xenograft models of BRAF V600E-positive melanoma, including models with BRAF-inhibitor resistance (PMID: 25873592). | 25873592 |
| BRAF V600E | colon cancer | sensitive | PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX4720 inhibited growth of colon cancer cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 18287029). | 18287029 |
| BRAF V600E | melanoma | sensitive | PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX4720 inhibited growth of melanoma cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 18287029). | 18287029 |
| BRAF V600E | glioblastoma | decreased response | PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated a decreased response to treatment with PLX4720, demonstrating increased viability of CD133 positive cells in culture and in xenograft models (PMID: 26573800). | 26573800 |
| BRAF V600E | Advanced Solid Tumor | sensitive | PLX4720 | Preclinical | Actionable | In a preclinical study, PLX4720 inhibited Erk phosphorylation and cell proliferation of transformed cells expression BRAF V600E in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | melanoma | sensitive | PLX4720 + Selumetinib | Preclinical | Actionable | In a preclinical study, PLX4720 and Selumetinib (AZD6244) worked synergistically to inhibit cell growth in PLX4720-resistant melanoma cell lines harboring BRAF V600E in culture (PMID: 26461489). | 26461489 |
| BRAF V600E | high grade glioma | predicted - sensitive | PLX4720 + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and PLX4720 synergistically inhibited growth and induced apoptosis in glioma cell lines in culture, resulted in prolonged survival in cell line xenograft models (PMID: 27217440). | 27217440 |
| BRAF V600E | neuroendocrine tumor | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in a rapid and sustained clinical response in a patient with a rectal neuroendocrine tumor harboring a BRAF V600E mutation (PMID: 27048246). | 27048246 |
| BRAF V600E | neuroendocrine tumor | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Mekinist (trametinib) and Tafinlar (dabrafenib) combination therapy is included in guidelines for patients with unresectable or metastatic extrapulmonary poorly differentiated neuroendocrine carcinoma, large or small cell carcinoma, or mixed neuroendocrine/non-neuroendocrine neoplasms harboring BRAF V600E who have progressed on or following prior treatment (NCCN.org). | detail... |
| BRAF V600E | hairy cell leukemia | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (ROAR), treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) demonstrated safety and resulted in an overall response rate of 89.1% (49/55; 36 complete responses, 13 partial responses) in patients with heavily pretreated recurrent/refractory hairy cell leukemia harboring BRAF V600E, with 24-month duration of response, progression-free-survival, and overall survival rates of 97.7%, 94.4% and 94.5%, respectively (PMID: 36108341; NCT02034110). | 36108341 |
| BRAF V600E | pancreatic cancer | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a retrospective analysis, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response in two patients with pancreatic cancer harboring BRAF V600E, including one patient with a progression-free survival (PFS) of at least 2 years on third-line therapy and another patient with a PFS of 48 weeks on second-line therapy (PMID: 34476331). | 34476331 |
| BRAF V600E | pancreatic endocrine carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response lasting at least 15 months in a patient with unresectable, metastatic pancreatic neuroendocrine carcinoma harboring BRAF V600E (PMID: 38814411). | 38814411 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial, BRAF V600E positive melanoma patients who progressed on treatment with BRAF inhibitors or the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) were treated again with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) after 12 weeks off treatment, which resulted in a partial response in 35% (8/25) and stable disease in 40% (10/25) (PMID: 28268064). | 28268064 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + Trametinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (COMBI-v) that supported FDA approval, the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in an improved overall survival rate at 12 months (72% vs 65%, HR=0.69, p=0.005), median progression-free survival (11.4 vs 7.3 months, HR=0.56, p<0.001), and objective response rate (64% vs 51%, p<0.001) compared to Zelboraf (vemurafenib) in melanoma patients harboring BRAF V600E or V600K (PMID: 25399551; NCT01597908). | detail... detail... 25399551 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + Trametinib | Preclinical | Actionable | In a preclinical study, Tafinlar (dabrafenib) in combination with Mekinist (trametinib) inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 22389471). | 22389471 |
| BRAF V600E | ovary epithelial cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as systemic therapy for patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | glomus tumor | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in decreased tumor size lasting at least 9 months in an adolescent (18 years old) patient with malignant glomus tumor harboring BRAF V600E (PMID: 30556047). | 30556047 |
| BRAF V600E | basal cell carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in stable disease after three months of treatment in a patient with basal cell carcinoma harboring BRAF V600E (PMID: 33537843) | 33537843 |
| BRAF V600E | acinar cell carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in near complete metabolic remission at 5 months and persistent complete metabolic remission at 12 months in a patient with metastatic acinar cell carcinoma of unknown primary harboring BRAF V600E (PMID: 38820503). | 38820503 |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines for patients with recurrent glioblastoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, an epithelioid glioblastoma patient harboring BRAF V600E treated with Mekinist (trametinib) and Tafinlar (dabrafenib) combination therapy resulted in stable disease, and the patient continued to demonstrate stable disease at least 16 months after initiation of therapy (PMID: 29632053). | 29632053 |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination therapy of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in improved clinical symptoms in a patient with epithelioid glioblastoma harboring BRAF V600E, and treatment of the patient's cells resulted in decreased cell viability, reduced phosphorylation of Mek and Erk, increased apoptotic activity compared to either agent alone, and cell cycle arrest in culture, and led to tumor growth suppression in the patient-derived xenograft (PDX) model (PMID: 31345255). | 31345255 |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in a complete resolution of symptoms and radiographic partial response after the first treatment in a patient with glioblastoma harboring BRAF V600E whose disease progressed on PLX8394 treatment, and a complete response after 11 months of treatment, CDKN2A/B loss and CHEK2 T367fs were also identified in the tumor (PMID: 32923904). | 32923904 |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in significant clinical improvement in a patient with epithelioid glioblastoma harboring BRAF V600E, however, her disease progressed after 3 months of therapy (PMID: 31217909). | 31217909 |
| BRAF V600E | glioblastoma | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (ROAR), Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in an objective response in 32% (10/31, 2 complete responses, 8 partial responses) and stable disease in 19% (6/31) of patients with glioblastoma harboring BRAF V600E (PMID: 34838156; NCT02034110). | 34838156 |
| BRAF V600E | high grade glioma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response in a pediatric patient with posterior fossa high grade glioma harboring BRAF V600E and deletion of CDKN2A (PMID: 39399174). | 39399174 |
| BRAF V600E | high grade glioma | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (ROAR), Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in an objective response rate of 33% (15/45, 3 complete responses, 12 partial responses) in patients with high-grade glioma harboring BRAF V600E, with a median duration of response of 36.9 months, a median progression-free survival of 3.8 months, and an overall survival of 17.6 months (PMID: 34838156; NCT02034110). | 34838156 |
| BRAF V600E | high grade glioma | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial, Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in an overall response rate of 56.1% (23/41; 12 complete, 11 partial responses), a clinical benefit rate of 65.9% (27/41), median duration of response of 22.2 months, median progression-free survival of 9.0 months, and median overall survival of 32.8 months in pediatric patients with relapsed or refractory high-grade glioma harboring BRAF V600E (PMID: 37643378; NCT02684058). | 37643378 |
| BRAF V600E | high grade glioma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as adjuvant therapy for pediatric patients with diffuse high-grade gliomas harboring BRAF V600E, or as a preferred regimen for patients with recurrent or progressive disease (NCCN.org). | detail... |
| BRAF V600E | brain glioblastoma multiforme | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy resulted in tumor shrinkage after 2 months in a patient with epithelioid glioblastoma multiforme harboring BRAF V600E, who had progressed after resection, radiotherapy, and chemotherapy, and following an interruption in therapy due to toxicity demonstrated a partial response and remained progression-free for 19 months, prior to progressing 29 months after initiation of therapy (PMID: 33461766). | 33461766 |
| BRAF V600E | anaplastic astrocytoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines for patients with recurrent anaplastic gliomas harboring BRAF V600E, including anaplastic astrocytoma (NCCN.org). | detail... |
| BRAF V600E | gallbladder cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as subsequent-line therapy for patients with biliary cancer harboring BRAF V600E, including gallbladder cancer (NCCN.org). | detail... |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Tafinlar (dabrafenib) and Mekinist (trametinib) led to a partial response after 1 month of treatment in a metastatic pancreatic ductal adenocarcinoma patient harboring BRAF V600E, followed by disease progression, which was detected 12 months later (PMID: 35382161). | 35382161 |
| BRAF V600E | ampulla of Vater adenocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as first-line therapy with good (ECOG 0-1; category 3) or poor (category 2B) performance status, or as subsequent therapy, for metastatic ampullary adenocarcinoma patients harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | esophagus squamous cell carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic esophageal squamous cell carcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | craniopharyngioma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response and progression-free survival of 1040 days in a patient with craniopharyngioma harboring BRAF V600E (PMID: 39143272). | 39143272 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines as a first-line or subsequent therapy for advanced or metastatic non-small cell lung cancer patients harboring BRAF V600E mutations (NCCN.org). | detail... |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Dabrafenib + Trametinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial that supported FDA approval, treatment with the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) in patients with non-small cell lung cancer harboring BRAF V600E resulted in an overall response rate of 66.7% (38/57) in previously treated patients and 64% (23/36) in untreated patients, versus 33% (26/78) treated with Tafinlar (dabrafenib) alone (PMID: 27080216, PMID: 27283860, PMID: 28919011; NCT01336634). | 27283860 detail... 27080216 detail... detail... 28919011 |
| BRAF V600E | lung adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response ongoing for at least 73 months in an elderly patient with lung adenocarcinoma harboring BRAF V600E (PMID: 39376796). | 39376796 |
| BRAF V600E | lung adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response with a decrease in the size of the lung lesion in a patient with metastatic lung adenocarcinoma harboring BRAF V600E and germline BRCA L1908Rfs*2, who had previously progressed on several lines of therapy (PMID: 38715777). | 38715777 |
| BRAF V600E | follicular thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | The combination of Tafinlar (dabrafenib) and Mekinist (trametinib) is included in guidelines for patients with follicular thyroid carcinoma harboring BRAF V600E who have progressed on therapy and have no further treatment options (NCCN.org). | detail... |
| BRAF V600E | thyroid gland carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in a partial response after 3 months in a patient with metastatic squamous cell carcinoma of the thyroid harboring BRAF V600E (PMID: 34956922). | 34956922 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, a papillary thyroid carcinoma patient who progressed on Lenvima (lenvatinib) was found to harbor BRAF V600E and was treated with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) on a clinical trial, resulting in partial response in the thyroid bed, cervical and intrathoracic lymph nodes, and pulmonary lesions, with a decrease in target lesion size of 67%, and the patient remained on treatment for 18 months before stopping due to progression (PMID: 31085763). | 31085763 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | The combination of Tafinlar (dabrafenib) and Mekinist (trametinib) is included in guidelines for patients with papillary thyroid carcinoma harboring BRAF V600E who have progressed on therapy and have no further treatment options (NCCN.org). | detail... |
| BRAF V600E | pancreatic adenocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as first-line therapy for patients with locally advanced (category 2A) or metastatic (category 2B) pancreatic adenocarcinoma harboring BRAF V600E, and as subsequent-line therapy for patients with locally advanced, recurrent, or metastatic disease (category 2A) (NCCN.org). | detail... |
| BRAF V600E | colon neuroendocrine neoplasm | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) resulted in a clinical improvement and reduction of the primary tumor as well as the metastatic lesions in a cecal neuroendocrine carcinoma patient harboring BRAF V600E (PMID: 30036245). | 30036245 |
| BRAF V600E | colon neuroendocrine neoplasm | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical study, second-line treatment with the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) resulted in a partial response in two patients with a neuroendocrine carcinoma of the colon harboring BRAF V600E, with progression-free survival of 6 months in one patient and 4 months in the second patient (PMID: 38716076). | 38716076 |
| BRAF V600E | biliary tract cancer | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (ROAR), Tafinlar (dabrafenib) in combination with Mekinist (trametinib) demonstrated a manageable safety profile and resulted in an overall response rate of 51% (22/43, all partial responses) in patients with biliary tract cancer harboring BRAF V600E, with a median duration of response of 9 months, a median progression-free survival of 9 months, and a median overall survival of 14 months (PMID: 32818466; NCT02034110). | 32818466 |
| BRAF V600E | biliary tract cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as second or later-line therapy for patients with biliary tract cancer harboring BRAF V600E (PMID: 36372281; ESMO.org). | 36372281 detail... |
| BRAF V600E | biliary tract cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as subsequent-line therapy for patients with biliary tract cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | breast metaplastic carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response in a patient with metaplastic breast cancer harboring BRAF V600E, however, progression occurred after 8 weeks (PMID: 32206360). | 32206360 |
| BRAF V600E | extrahepatic bile duct carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as subsequent-line therapy for patients with biliary cancer harboring BRAF V600E, including extrahepatic cholangiocarcinoma (NCCN.org). | detail... |
| BRAF V600E | pilocytic astrocytoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines as an adjuvant treatment for patients with pilocytic astrocytoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | pilocytic astrocytoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, the addition of Mekinist (trametinib) to treatment with Tafinlar (dabrafenib) resulted in a partial response in 3 pediatric patients with suprasellar pilocytic astrocytoma harboring BRAF V600E who all previously progressed on Tafinlar (dabrafenib) treatment alone (PMID: 39399174). | 39399174 |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in clinical benefit that lasted for more than 14 months in a patient with pleomorphic xanthoastrocytoma harboring BRAF V600E (PMID: 29632053). | 29632053 |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Mekinist (trametinib) and Tafinlar (dabrafenib) combination therapy is included in guidelines as an adjuvant treatment for patients with pleomorphic xanthoastrocytoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | small intestine adenocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines for patients with advanced or metastatic small bowel adenocarcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | esophagus adenocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic esophageal adenocarcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | intrahepatic cholangiocarcinoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Tafinlar (dabrafenib) and Mekinist (trametinib) in a patient with intrahepatic cholangiocarcinoma harboring BRAF V600E who progressed on chemotherapy led to stable disease at 6 weeks, improvement of lung and liver lesions at 12 weeks after treatment, and response was maintained until disease progression in the liver was observed at 10 months (PMID: 33537843). | 33537843 |
| BRAF V600E | intrahepatic cholangiocarcinoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in an objective response rate of 38% in patients with advanced solid tumors harboring BRAF V600E, with a significantly greater tumor shrinkage observed in patients (n=4) with intrahepatic cholangiocarcinoma compared to the trial average ( -60% vs -35%, P=0.016) (PMID: 38109210). | 38109210 |
| BRAF V600E | intrahepatic cholangiocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as subsequent-line therapy for patients with biliary cancer harboring BRAF V600E, including intrahepatic cholangiocarcinoma (NCCN.org). | detail... |
| BRAF V600E | gastroesophageal junction adenocarcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic gastroesophageal junction adenocarcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | cholangiocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Tafinlar (dabrafenib) and Mekinist (trametinib) in a patient with metastatic cholangiocarcinoma harboring BRAF V600E who progressed on chemotherapy led to a sustained metabolic response for six months (PMID: 33537843). | 33537843 |
| BRAF V600E | ganglioglioma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines as an adjuvant treatment for patients with ganglioglioma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | renal Wilms' tumor | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical study, combination treatment with Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in regression in the metastatic disease of the liver, spleen, and peritoneum along with clinical symptom improvement in an adult patient with metastatic Wilms' tumor harboring BRAF V600E (PMID: 39234402). | 39234402 |
| BRAF V600E | epithelial predominant Wilms' tumor | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy resulted in a complete radiographic response 4 months after treatment initiation that was maintained for at least 12 months in a pediatric patient with metastatic epithelial-predominant Wilms tumor harboring BRAF V600E (PMID: 32238401). | 32238401 |
| BRAF V600E | lung papillary adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in regression of the lesions in the chest, abdomen and brain in a patient with lung papillary carcinoma harboring BRAF V600E but progression was observed 3 months later (PMID: 34178685). | 34178685 |
| BRAF V600E | pancreatic acinar cell adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Tafinlar (dabrafenib) and Mekinist (trametinib) in a patient with pancreatic acinar cell carcinoma harboring BRAF V600E who had previously progressed on chemotherapy led to a response at 8 weeks, and ongoing clinical and radiological response was still observed at 32 months of treatment (PMID: 33537843). | 33537843 |
| BRAF V600E | pancreatic acinar cell adenocarcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in near complete remission allowing for debulking surgery and disease control for 12 months in a patient with metastatic pancreatic acinar cell carcinoma harboring BRAF V600E, along with germline PALB2 R414* (PMID: 32843432). | 32843432 |
| BRAF V600E | anaplastic oligodendroglioma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines for patients with recurrent anaplastic gliomas harboring BRAF V600E, including anaplastic oligodendroglioma (NCCN.org). | detail... |
| BRAF V600E | lung combined large cell neuroendocrine carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a partial response after 10 weeks in a patient with combined large cell neuroendocrine carcinoma harboring BRAF V600E, who remained recurrence-free for at least a year (PMID: 34969785). | 34969785 |
| BRAF V600E | oncocytic carcinoma of the thyroid | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | The combination of Tafinlar (dabrafenib) and Mekinist (trametinib) is included in guidelines for patients with thryoid Hürthle cell carcinoma harboring BRAF V600E who have progressed on therapy and have no further treatment options (NCCN.org). | detail... |
| BRAF V600E | salivary gland cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines for patients with recurrent, unresectable, or metastatic salivary gland tumors harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | skin melanoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines for cutaneous melanoma patients harboring a BRAF V600 mutation, such as BRAF V600E, as neoadjuvant or adjuvant therapy for stage III disease and as systemic therapy for patients with unresectable or metastatic disease (NCCN.org). | detail... |
| BRAF V600E | gastrointestinal stromal tumor | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) in combination with Mekinist (trametinib) is included in guidelines as neoadjuvant therapy for patients with resectable disease and as first-line systemic therapy for patients with unresectable or metastatic gastrointestinal stromal tumor (GIST) harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Trametinib | Phase Ib/II | Actionable | In a Phase Ib/II trial, treatment with the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) resulted in partial response or better in 12% (5/43), including 1 complete response, and stable disease in 51% (22/43) of patients with colorectal cancer harboring BRAF V600E (PMID: 26392102). | 26392102 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Tafinlar (dabrafenib) and Mekinist (trametinib) inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | stomach cancer | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines as second-line or subsequent therapy for patients with unresectable locally advanced, recurrent, or metastatic gastric cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | spermatic cord cancer | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a regression of the lung metastasis and progression-free survival of 6.5 months in a patient with undifferentiated sarcoma of the spermatic cord harboring BRAF V600E (PMID: 36157689). | 36157689 |
| BRAF V600E | large cell neuroendocrine carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) resulted in a partial response in one of the lesions and a complete response in other lesions after 1 month in a patient with large cell neuroendocrine carcinoma of unknown primary harboring BRAF V600E (PMID: 36847048). | 36847048 |
| BRAF V600E | salivary gland carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case report, combined Tafinlar (dabrafenib) and Mekinist (trametinib) treatment of a patient with salivary duct carcinoma harboring BRAF V600E resulted in a reduction of metastatic lesions and stable disease lasting 13 months followed by disease progression (PMID: 30323086). | 30323086 |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy resulted in a complete response after 8 months of treatment in a patient with low-grade serous ovarian carcinoma harboring BRAF V600E (PMID: 33043759). | 33043759 |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in a partial response lasting at least 2.5 years in one patient with low grade serous ovarian carcinoma harboring BRAF V600E, and resulted in a complete metabolic response after 4 months of treatment in a second patient (PMID: 35242981). | 35242981 |
| BRAF V600E | Her2-receptor negative breast cancer | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a complete response in the liver and bone lesions with a progression-free survival of 9 months in a patient with metastatic ERBB2 (HER2)-negative, hormone receptor-positive breast cancer harboring BRAF V600E (PMID: 36531075). | 36531075 |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in a clinical and radiologic response that lasted for 9 months in an anaplastic thyroid cancer patient harboring BRAF V600E (PMID: 27697975). | 27697975 |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Dabrafenib + Trametinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial (ROAR) that supported FDA approval, the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in an overall response rate of 61% (20/33; 3 complete responses, 17 partial responses) in patients with anaplastic thyroid cancer harboring BRAF V600E, with 12-month duration of response rate of 50%, a median progression-free survival and overall survival of 6.7 and 14.5 months, respectively (PMID: 35026411; NCT02034110). | 35026411 detail... detail... detail... |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines for metastatic thyroid gland anaplastic carcinoma patients harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy is included in guidelines for patients with advanced or metastatic thyroid gland anaplastic carcinoma harboring BRAF V600E (PMID: 31549998, PMID: 35491008; ESMO.org). | 31549998 detail... 35491008 |
| BRAF V600E | low grade glioma | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | Combination of Mekinist (trametinib) and Tafinlar (dabrafenib) is included in guidelines for patients with recurrent or progressive low grade glioma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | low grade glioma | sensitive | Dabrafenib + Trametinib | Phase Ib/II | Actionable | In a Phase I/II trial (Study X2101), Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment demonstrated manageable toxicity and resulted in an objective response rate of 25% (9/36, 1 complete response, 8 partial responses) and stable disease in 67% (24/36) of pediatric patients with pretreated low-grade glioma harboring BRAF V600E (J Clin Oncol 38, no. 15_suppl (May 20, 2020) 10506; NCT02124772). | detail... |
| BRAF V600E | low grade glioma | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (ROAR), Tafinlar (dabrafenib) and Mekinist (trametinib) combination treatment resulted in an objective response rate of 69% (9/13, 1 complete response, 6 partial responses, 2 minor responses) in patients with low-grade glioma harboring BRAF V600E, with median duration of response, median progression-free survival, and overall survival time unreached (PMID: 34838156; NCT02034110). | 34838156 |
| BRAF V600E | low grade glioma | sensitive | Dabrafenib + Trametinib | FDA approved | Actionable | In a Phase II trial that supported FDA approval, Mekinist (trametinib) plus Tafinlar (dabrafenib) significantly improved overall response rate (47% vs 11%, risk ratio 4.31, p<0.001), clinical benefit rate (86% vs 46%), median progression-free survival (PFS, 20.1 vs 7.4 months, p<0.001, HR 0.31), and 12-month PFS rate (67% vs 26%) compared to standard chemotherapy in pediatric patients of 1 year and older with low-grade glioma harboring BRAF V600E (PMID: 37733309; NCT02684058). | detail... detail... 37733309 |
| BRAF V600E | anaplastic pleomorphic xanthoastrocytoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Tafinlar (dabrafenib) combination treatment resulted in an ongoing partial response 8 months after initiation of treatment in a patient with anaplastic pleomorphic xanthoastrocytoma harboring BRAF V600E, and a near complete response after 3 months of treatment in another patient with relapsed disease (PMID: 28984141). | 28984141 |
| BRAF V600E | IDH-wildtype glioblastoma | predicted - sensitive | Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy resulted in a partial response lasting 9 months in a patient with metastatic MGMT unmethylated, IDH-wildtype glioblastoma harboring BRAF V600E along with amplification of MYC and TERT and loss of CDKN2A/B (PMID: 36825105). | 36825105 |
| BRAF V600E | Advanced Solid Tumor | sensitive | Dabrafenib + Trametinib | FDA approved | Actionable | In 3 Phase II trials (ROAR, NCI-MATCH, X2101) that supported FDA approval, Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy demonstrated safety and efficacy in adult and pediatric (6 years or older) patients with advanced solid tumors harboring BRAF V600E (PMID: 34838156, PMID: 32818466, J Clin Oncol 37, no. 15_suppl (May 20, 2019) 3002, J Clin Oncol 38, no. 15_suppl (May 20, 2020) 10506; NCT02034110, NCT02465060, NCT02124772). | 32818466 detail... detail... 34838156 detail... detail... |
| BRAF V600E | Advanced Solid Tumor | sensitive | Dabrafenib + Trametinib | Phase II | Actionable | In a Phase II trial (NCI-MATCH), Tafinlar (dabrafenib) and Mekinist (trametinib) combination therapy resulted in an objective response rate of 33.3% (11/33) in patients with advanced solid tumors other than melanoma, thyroid, colorectal, and lung cancer harboring BRAF V600E, with a median duration of response of 12 months, median progression-free survival of 9.4 months, and median overall survival not reached (J Clin Oncol 37, no. 15_suppl (May 20, 2019) 3002; NCT02465060). | detail... |
| BRAF V600E | Adenocarcinoma of Unknown Primary | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | The combination of Tafinlar (dabrafenib) and Mekinist (trametinib) is included in guidelines for patients with adenocarcinoma of unknown primary harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | Squamous Cell Carcinoma of Unknown Primary | sensitive | Dabrafenib + Trametinib | Guideline | Actionable | The combination of Tafinlar (dabrafenib) and Mekinist (trametinib) is included in guidelines for patients with squamous cell carcinoma of unknown primary harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | melanoma | sensitive | AZ628 | Preclinical - Cell culture | Actionable | In a preclinical study, AZ628 inhibited proliferation of melanoma cell lines harboring either monomeric BRAF V600E or dimeric isoform of V600E which conferred Zelboraf (vemurafenib)-resistance in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | colon cancer | sensitive | GDC0879 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, GDC0879 inhibited survival of colon cancer cell lines harboring BRAF V600E in cell culture and cell line xenograft models (PMID: 19276360). | 19276360 |
| BRAF V600E | melanoma | sensitive | GDC0879 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, GDC0879 inhibited survival of melanoma cell lines harboring BRAF V600E in cell culture, cell line xenograft and patient-derived xenograft (PDX) models (PMID: 19276360). | 19276360 |
| BRAF V600E | thyroid cancer | sensitive | Binimetinib + Encorafenib | Phase II | Actionable | In a Phase II trial, treatment with Mektovi (binimetinib) plus Braftovi (encorafenib) demonstrated safety and activity in patients with BRAF V600E-mutant thyroid cancer, regardless of histological subtype, resulting in an objective response rate of 54.5% (12/22, 12 partial responses), disease control rate of 100% (22/22), and 12-month rate of ongoing response of 90.9%, and median duration of response, median progression-free survival, and median overall survival were not reached (PMID: 38343359). | 38343359 |
| BRAF V600E | malignant fibrous histiocytoma | sensitive | Binimetinib + Encorafenib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mektovi (binimetinib) and Braftovi (encorafenib) resulted in a clinical response after two months in a patient with angiomatoid fibrous histiocytoma harboring BRAF V600E, along with EWSR1-CREB1 (e7:e7), and in a preclinical study, combination treatment with Mektovi (binimetinib) and Braftovi (encorafenib) inhibited viability of cells in culture (PMID: 38885476). | 38885476 |
| BRAF V600E | melanoma | sensitive | Binimetinib + Encorafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III (COLUMBUS) trial that supported FDA approval, Braftovi (encorafenib) in combination with Mektovi (binimetinib) demonstrated improved tolerability profile and efficacy, resulted in a progression-free survival of 14.9 months in patients with advanced melanoma harboring BRAF V600E/K mutations, comparing to 7.3 months in the Zelboraf (vemurafenib) group (HR=0.54, p<0.0001) (PMID: 29573941; NCT01909453), and both BRAF V600E and V600K are on the companion diagnostic. | 29573941 detail... detail... detail... |
| BRAF V600E | melanoma | sensitive | Binimetinib + Encorafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III (COLUMBUS) trial that supported FDA approval, Braftovi (encorafenib) in combination with Mektovi (binimetinib) resulted in a median overall survival (OS) of 33.6 months, a 1-year OS rate of 77.5%, and a 2-year OS rate of 57.7% in patients with advanced melanoma harboring BRAF V600E/K mutations compared to a median OS of 16.9 months and 1- and 2-year OS rates of 63.1% and 43.2%, respectively, in the Zelboraf (vemurafenib) treated group (PMID: 30219628; NCT01909453). | detail... 30219628 detail... detail... |
| BRAF V600E | glomus tumor | predicted - sensitive | Binimetinib + Encorafenib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mektovi (binimetinib) and Braftovi (encorafenib) resulted in a complete response lasting more than 2 years in a patient with metastatic malignant glomus tumor harboring BRAF V600E (PMID: 39392364). | 39392364 |
| BRAF V600E | high grade glioma | sensitive | Binimetinib + Encorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, treatment with the combination of Mektovi (binimetinib) and Braftovi (encorafenib) demonstrated safety and activity in patients with high grade glioma harboring BRAF V600E, resulting in a radiographic response rate of 60% (3/5, 1 complete and 2 partial responses), with stable disease in 1 patient, a median duration of response of 10 months, a median progression-free survival of 9.4 months, and a median overall survival of 14.6 months (PMID: 38446982; NCT03973918). | 38446982 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Binimetinib + Encorafenib | Guideline | Actionable | Combination of Braftovi (encorafenib) and Mektovi (binimetinib) is included in guidelines as a first-line or subsequent therapy for advanced or metastatic non-small cell lung cancer patients harboring BRAF V600E mutations (NCCN.org). | detail... |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Binimetinib + Encorafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial (PHAROS) that supported FDA approval, Braftovi (encorafenib) and Mektovi (binimetinib) combination therapy resulted in an objective response rate (ORR) of 75% (44/59; 9 complete, 35 partial responses) with a duration of response (DOR) lasting 12 or more months in 59% of treatment-naive patients, and an ORR of 46% (18/39) with a DOR lasting 12 or more months in 33% of previously treated patients with metastatic non-small cell lung cancer harboring BRAF V600E (PMID: 37270692; NCT03915951). | detail... detail... detail... 37270692 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Binimetinib + Encorafenib | Phase II | Actionable | In a Phase II trial, Mektovi (binimetinib) plus Braftovi (encorafenib) demonstrated safety in patients with BRAF V600E-mutant thyroid cancer and resulted in an objective response rate (ORR) of 54.5% (12/22, 12 partial responses (PR)), with an ORR of 47.1% (8/17, 8 PR) and a disease control rate of 100% (17/17) in the differentiated thyroid cancer cohort (all papillary thyroid cancer), and median duration of response, progression-free survival, and overall survival were not reached (PMID: 38343359). | 38343359 |
| BRAF V600E | skin melanoma | sensitive | Binimetinib + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Mektovi (binimetinib) is included in guidelines as first-line and second-line therapy for patients with metastatic or unresectable cutaneous melanoma harboring BRAF V600E or V600K mutations (PMID: 30959471; NCCN.org). | detail... 30959471 |
| BRAF V600E | multiple myeloma | sensitive | Binimetinib + Encorafenib | Phase II | Actionable | In a Phase II trial (BIRMA), Mektovi (binimetinib) plus Braftovi (encorafenib) treatment demonstrated safety and efficacy in relapsed/refractory multiple myeloma patients with BRAF V600E, with an overall response rate of 83% (10/12, 1 complete response (CR), 2 near-CR, 6 very good partial responses (PR), and 1 PR), a median duration of response of 4.8 mo, a median progression-free survival of 5.6 mo, and a median overall survival not reached but 66% at 12 mo and 55% at 24 mo (PMID: 36608320; NCT02834364). | 36608320 |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | Binimetinib + Encorafenib | Case Reports/Case Series | Actionable | In a clinical case study, Braftovi (encorafenib) and Mektovi (binimetinib) combination therapy resulted in durable stable disease lasting at least 3.5 years in a patient with low-grade serous ovarian carcinoma harboring BRAF V600E, who was previously treated with the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) (PMID: 33043759). | 33043759 |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Binimetinib + Encorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, Mektovi (binimetinib) and Braftovi (encorafenib) combination therapy demonstrated safety and activity in patients with thyroid cancer harboring BRAF V600E, resulting in an objective response rate (ORR) of 54.5% (12/22, 12 partial responses (PR)), with an ORR of 80% (4/5, 4 PR) and a disease control rate of 100% (5/5) in patients with anaplastic thyroid cancer, and median duration of response, progression-free survival, and overall survival were not reached (PMID: 38343359). | 38343359 |
| BRAF V600E | Advanced Solid Tumor | predicted - sensitive | Binimetinib + Encorafenib | Phase II | Actionable | In a Phase II trial (BELIEVE), treatment with the combination of Braftovi (encorafenib) and Mektovi (binimetinib) resulted in an objective response rate of 32.7%, median progression-free survival (PFS) of 4.8 months, and 6-month PFS rate of 37.5% in patients with advanced solid tumors harboring BRAF V600E (n=43), other BRAF mutation (n=5), or a BRAF fusion (n=1) (Ann Oncol (2024) 35 (Suppl_2): S497). | detail... |
| BRAF V600E | lung non-small cell carcinoma | not predictive | Atezolizumab | Clinical Study - Cohort | Actionable | In a retrospective analysis, non-small cell lung cancer patients harboring BRAF V600E did not demonstrate a significantly different response to treatment with either Keytruda (pembrolizumab), Opdivo (nivolumab), or Tecentriq (atezolizumab) compared to patients with BRAF non-V600E mutations, demonstrating an objective response rate of 25% (3/12) vs 33% (3/9) (p=1.0) and median progression-free survival of 3.7 months vs 4.1 months (p=0.37) (PMID: 29723688). | 29723688 |
| BRAF V600E | melanoma | sensitive | Encorafenib + Ribociclib | Phase Ib/II | Actionable | In a Phase Ib/II trial, Encorafenib (LGX818) and Kisqali (ribociclib) combination treatment resulted in confirmed partial response in 7.1% (2/28), unconfirmed partial response in 10.7% (3/28), and stable disease in 35.7% (10/28) of patients with melanoma harboring BRAF V600E (PMID: 28351928). | 28351928 |
| BRAF V600E | endometrial adenocarcinoma | predicted - sensitive | Dabrafenib + Rabeprazole + Rifampin | Case Reports/Case Series | Actionable | In a Phase I trial, combination treatment with Tafinlar (dabrafenib), Rabeprazole, and Rifampin in a patient with metastatic endometrial adenocarcinoma harboring BRAF V600E, that recurred 11 years after original diagnosis and was refractory to treatment with chemotherapy, led to reduction of lung metastases and pelvic tissue mass at three months, but a slight increase in pelvic mass was observed at six months (PMID: 33537843; NCT01954043). | 33537843 |
| BRAF V600E | melanoma | decreased response | Nivolumab | Clinical Study - Cohort | Actionable | In a retrospective analysis, patients with melanoma harboring BRAF V600E (n=84) had decreased response rates (29% vs. 53%, p=0.059), progression-free survival (2.7 vs. 19 months, p=0.049), and overall survival (11.7 vs. 20.4 months, p=0.081) relative to patients with BRAF V600K (n=19) when treated with Keytruda (pembrolizumab) (n=62 and 17 for BRAF V600E and V600K, respectively) or Opdivo (nivolumab) (n=22 and 2 for BRAF V600E and V600K, respectively) (PMID: 30630828). | 30630828 |
| BRAF V600E | lung non-small cell carcinoma | not predictive | Nivolumab | Clinical Study - Cohort | Actionable | In a retrospective analysis, non-small cell lung cancer patients harboring BRAF V600E did not demonstrate a significantly different response to treatment with either Keytruda (pembrolizumab), Opdivo (nivolumab), or Tecentriq (atezolizumab), compared to patients with BRAF non-V600E mutations, demonstrating an objective response rate of 25% (3/12) vs 33% (3/9) (p=1.0) and median progression-free survival of 3.7 months vs 4.1 months (p=0.37) (PMID: 29723688). | 29723688 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Irinotecan + Vemurafenib | Phase II | Actionable | In a Phase II trial (SWOG1406), addition of Zelboraf (vemurafenib) to Camptosar (irinotecan) plus Erbitux (cetuximab) improved progression-free survival (4.4 vs. 2.0 mo, HR 0.50, p=0.001), response rate (17% vs 4%, p=0.05), and disease control rate (67% vs. 22%, p<0.001) in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 33356422; NCT02164916). | 33356422 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Irinotecan + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with Erbitux (cetuximab) and Camptosar (irinotecan) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 22180495). | 22180495 |
| BRAF V600E | colon cancer | sensitive | Navitoclax + Trametinib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Mekinist (trametinib) on human colon cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | sensitive | Navitoclax + Trametinib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Mekinist (trametinib) on human melanoma cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Navitoclax + Trametinib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Mekinist (trametinib) on human non-small cell lung cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | decreased response | Pembrolizumab | Clinical Study | Actionable | In a retrospective analysis, patients with melanoma harboring BRAF V600E (n=84) had decreased response rates (29% vs. 53%, p=0.059), progression-free survival (2.7 vs. 19 months, p=0.049), and overall survival (11.7 vs. 20.4 months, p=0.081) relative to patients with BRAF V600K (n=19) when treated with Keytruda (pembrolizumab) (n=62 and 17 for BRAF V600E and V600K, respectively) or Opdivo (nivolumab) (n=22 and 2 for BRAF V600E and V600K, respectively) (PMID: 30630828). | 30630828 |
| BRAF V600E | melanoma | decreased response | Pembrolizumab | Clinical Study | Actionable | In a retrospective analysis, real-world treatment with either Keytruda (pembrolizumab) or Toripalimab (JS001) resulted in a median disease-free survival of 17 months in melanoma patients harboring BRAF V600E compared to 32 months in patients with wild-type BRAF, NRAS, and KIT (p=0.022) (PMID: 37403699). | 37403699 |
| BRAF V600E | lung non-small cell carcinoma | not predictive | Pembrolizumab | Clinical Study - Cohort | Actionable | In a retrospective analysis, non-small cell lung cancer patients harboring BRAF V600E did not demonstrate a significantly different response to treatment with either Keytruda (pembrolizumab), Opdivo (nivolumab), or Tecentriq (atezolizumab), compared to patients with BRAF non-V600E mutations, demonstrating an objective response rate of 25% (3/12) vs 33% (3/9) (p=1.0) and median progression-free survival of 3.7 months vs 4.1 months (p=0.37) (PMID: 29723688). | 29723688 |
| BRAF V600E | melanoma | predicted - sensitive | Dabrafenib + Pembrolizumab + Trametinib | Phase II | Actionable | In a Phase II trial (IMPemBra), Keytruda (pembrolizumab) in combination with short-term or intermittent Tafinlar (dabrafenib) plus Mekinist (trametinib) resulted in improved median progression-free survival compared to Keytruda (pembrolizumab) monotherapy (27.0 vs 10.6 mo, p=0.13) in patients with treatment-naive advanced melanoma harboring BRAF V600E (n=26) or V600K (n=6) mutations (J Clin Oncol 38: 2020 (suppl; abstr 10021); NCT02625337). | detail... |
| BRAF V600E | skin melanoma | sensitive | Dabrafenib + Pembrolizumab + Trametinib | Guideline | Actionable | Tafinlar (dabrafenib) plus Mekinist (trametinib) in combination with an immune checkpoint inhibitor, such as Keytruda (pembrolizumab), is included in guidelines as second-line or subsequent therapy (category 2A) for patients with metastatic or unresectable cutaneous melanoma harboring a BRAF V600 mutation, such as BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | melanoma | predicted - resistant | KRT-232 | Preclinical - Pdx | Actionable | In a preclinical study, patient-derived xenograft (PDX) models of melanoma harboring BRAF V600E demonstrated resistance to treatment with KRT-232 (AMG 232) (PMID: 32234759). | 32234759 |
| BRAF V600E | melanoma | predicted - sensitive | Dabrafenib + KRT-232 + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, the addition of KRT-232 (AMG 232) to the combination treatment of Tafinlar (dabrafenib) and Mekinist (trametinib) resulted in a synergistic effect, leading to a greater decrease in tumor growth and tumor size compared to either KRT-232 (AMG 232) alone or Tafinlar (dabrafenib) plus Mekinist (trametinib) in patient-derived xenograft (PDX) models of melanoma harboring BRAF V600E (PMID: 32234759). | 32234759 |
| BRAF V600E | breast cancer | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a complete response that lasted 170 days and 2 partial responses out of 4 patients with advanced breast cancer harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | pancreatic cancer | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in 2 patients with pancreatic cancer harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | pancreatic endocrine carcinoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in a patient with pancreatic neuroendocrine carcinoma harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | melanoma | sensitive | Cobimetinib + Vemurafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (coBRIM) that supported FDA approval, treatment with the combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) resulted in an improved progression-free survival of 12.3 months, compared to 7.2 months with Zelboraf (vemurafenib) plus placebo, among patients with BRAF V600-mutated metastatic melanoma, and BRAF V600E and BRAF V600K are on the companion diagnostic (PMID: 27480103; NCT01689519). | 27480103 detail... detail... |
| BRAF V600E | ovarian cancer | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in one complete response lasting 5 weeks, 2 partial responses, and 1 with stable disease lasting more than 16 weeks out of 6 patients with advanced ovarian cancer harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | breast malignant phyllodes tumor | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in a patient with a phyllodes tumor of the breast harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | glioblastoma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) is included in guidelines for patients with recurrent glioblastoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | glioblastoma | sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with epithelioid glioblastoma harboring BRAF V600E continued to response as Cotellic (cobimetinib) was added to Zelboraf (vemurafenib) treatment (PMID: 31217909). | 31217909 |
| BRAF V600E | anaplastic astrocytoma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) is included in guidelines for patients with recurrent anaplastic gliomas harboring BRAF V600E, including anaplastic astrocytoma (NCCN.org). | detail... |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Cotellic (cobimetinib) and Zelboraf (vemurafenib) led to a partial response after 1 month of treatment in a microsatellite stable pancreatic ductal adenocarcinoma patient with BRAF V600E and amplification of FGFR1 and NOTCH2, with significant decrease in hepatic metastatic lesions and undetectable lung lesions at 6 months, and a progression-free survival of at least 6 months (PMID: 35382161). | 35382161 |
| BRAF V600E | colon neuroendocrine neoplasm | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in a patient with neuroendocrine carcinoma of the colon harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | clear cell sarcoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in a patient with clear cell sarcoma harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | large cell carcinoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical study, a patient with poorly differentiated large cell carcinoma harboring BRAF V600E experienced a complete response lasting at least 2 years on combination treatment with Cotellic (cobimetinib) and Zelboraf (vemurafenib) (PMID: 35046062). | 35046062 |
| BRAF V600E | pilocytic astrocytoma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy is included in guidelines as an adjuvant treatment for patients with pilocytic astrocytoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy is included in guidelines as an adjuvant treatment for patients with pleomorphic xanthoastrocytoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | cholangiocarcinoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination treatment resulted in reduction of the pulmonary nodules and hepatic lesions 6 months after treatment initiation in a patient with metastatic cholangiocarcinoma harboring BRAF V600E, who maintained a stable disease and remained on treatment at 20 months (PMID: 33669326). | 33669326 |
| BRAF V600E | cholangiocarcinoma | predicted - sensitive | Cobimetinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial (TAPUR), Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy resulted in a partial response in a patient with cholangiocarcinoma harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | ganglioglioma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy is included in guidelines as an adjuvant treatment for patients with ganglioglioma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | anaplastic oligodendroglioma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) is included in guidelines for patients with recurrent anaplastic gliomas harboring BRAF V600E, including anaplastic oligodendroglioma (NCCN.org). | detail... |
| BRAF V600E | skin melanoma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) and Cotellic (cobimetinib) combination therapy is included in cutaneous melanoma guidelines for patients with metastatic or unresectable disease harboring a BRAF V600 activating mutation (NCCN.org). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Cobimetinib + Vemurafenib | Phase II | Actionable | In a Phase II trial (TAPUR), the combination of Cotellic (cobimetinib) and Zelboraf (vemurafenib) resulted in an objective response rate of 30% (8/27; all partial responses), a disease control rate of 52% (14/27), a median progression-free survival of 15.7 weeks, and a median overall survival of 38.9 weeks in patients with colorectal cancer harboring BRAF V600E (n=26) or K601E (n=1) (PMID: 36409971; NCT02693535). | 36409971 |
| BRAF V600E | colorectal cancer | sensitive | Cobimetinib + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Cotellic (cobimetinib) and Zelboraf (vemurafenib) inhibited tumor growth in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 28649441). | 28649441 |
| BRAF V600E | low grade glioma | sensitive | Cobimetinib + Vemurafenib | Guideline | Actionable | Combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) is included in guidelines for patients with recurrent or progressive low grade glioma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | Advanced Solid Tumor | sensitive | Cobimetinib + Vemurafenib | Phase II | Actionable | In a Phase II trial (TAPUR), treatment with the combination of Zelboraf (vemurafenib) and Cotellic (cobimetinib) resulted in an objective response rate of 57% (16/28, 2 complete responses (CR), 14 partial responses (PR)) and a disease control rate (CR + PR + stable disease at 16 wks (SD16+)) of 68% in patients with advanced solid tumors harboring BRAF mutations, with 2 CR, 13 PR, and 2 SD16+ in a total of 26 patients harboring BRAF V600E (PMID: 38096472; NCT02693535). | 38096472 |
| BRAF V600E | colorectal cancer | sensitive | Pimasertib + Sorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 23629727). | 23629727 |
| BRAF V600E | melanoma | sensitive | Ganetespib + TAK-733 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the Hsp90 inhibitor Ganetespib in combination with the MEK1/2 inhibitor TAK-733 resulted in tumor regression in Zelboraf (vemurafenib)-resistant cell line xenograft models of melanoma harboring BRAF V600E (PMID: 24398428). | 24398428 |
| BRAF V600E | thyroid cancer | sensitive | Lapatinib + Vemurafenib | Preclinical | Actionable | In a preclinical study, the combination of Tykerb (lapatinib) and Zelboraf (vemurafenib) inhibited growth of thyroid cancer cells harboring a BRAF V600E mutation in culture and in BRAF-mutant mouse models of thyroid cancer (PMID: 23365119). | 23365119 |
| BRAF V600E | colorectal cancer | sensitive | Lapatinib + Panobinostat | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) and Faridak (panobinostat) worked synergistically to inhibit growth of BRAF V600E mutant colorectal cancer cells in culture (PMID: 21464044). | 21464044 |
| BRAF V600E | colorectal cancer | sensitive | Gefitinib + Vemurafenib | Preclinical | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Iressa (gefitinib) decreased the number of viable colorectal cancer cells harboring a BRAF V600E mutation in cell culture (PMID: 22448344). | 22448344 |
| BRAF V600E | colorectal cancer | sensitive | Erlotinib + Vemurafenib | Phase Ib/II | Actionable | In a Phase Ib/II trial (EVICT), the combination of Zelboraf (vemurafenib) and Tarceva (erlotinib) resulted in an overall response rate of 16% (5/31; 5 partial responses), a clinical benefit rate of 65% (20/31), a median progression-free survival of 3.9 months, and a median overall survival of 6.3 months in patients with colorectal cancer harboring BRAF V600E (PMID: 36638198). | 36638198 |
| BRAF V600E | colorectal cancer | sensitive | Erlotinib + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Tarceva (erlotinib) resulted in improved inhibition of tumor growth in BRAF V600E mutant human colon cancer cell line xenograft models compared to either drug as monotherapy (PMID: 22448344). | 22448344 |
| BRAF V600E | colorectal cancer | sensitive | Erlotinib + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with Tarceva (erlotinib) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E compared to either agent alone (PMID: 22180495). | 22180495 |
| BRAF V600E | Advanced Solid Tumor | predicted - sensitive | Erlotinib + Vemurafenib | Case Reports/Case Series | Actionable | In a Phase Ib/II trial (EVICT), the combination of Zelboraf (vemurafenib) and Tarceva (erlotinib) resulted in an overall response rate of 43% (3/7), a clinical benefit rate of 100%, and a median PFS of 5.5 months in patients with advanced solid tumors other tan colorectal cancer harboring BRAF V600E (PMID: 36638198). | 36638198 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, the combination of Zelboraf (vemurafenib) and Erbitux (cetuximab) was tolerated and showed clinical benefit in a patient with BRAF V600E mutant colorectal cancer (PMID: 24523613). | 24523613 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Zelboraf (vemurafenib) and Erbitux (cetuximab) combination treatment inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with Erbitux (cetuximab) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 22180495). | 22180495 |
| BRAF V600E | colorectal cancer | sensitive | Panitumumab + Vemurafenib | Phase I | Actionable | In a Phase I trial, 83% (10/12) of patients with colorectal cancer carrying a BRAF V600E mutation demonstrated tumor regression when treated with a combination of Zelboraf (vemurafenib) and Vectibix (panitumumab) (PMID: 25589621). | 25589621 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Panitumumab | Phase I | Actionable | In a Phase I trial, combination therapy consisting of Tafinlar (dabrafenib) and Vectibix (panitumumab) resulted in an overall response rate of 10% (2/20, 1 complete response, 1 partial response), stable disease in 80% (16/20), and a median progression-free survival of 3.5 months in patients with BRAF V600E colorectal cancer (PMID: 29431699; NCT01750918). | 29431699 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Panitumumab | Phase Ib/II | Actionable | In a Phase Ib/II trial, treatment with the combination of Vectibix (panitumumab) and Tafinlar (dabrafenib) resulted in stable disease in 7/8 colorectal cancer patients harboring a BRAF V600E mutation (J Clin Oncol 32:5s, 2014 (suppl; abstr 3515)). | detail... |
| BRAF V600E | high grade glioma | no benefit | ZM336372 | Preclinical - Patient cell culture | Actionable | In a preclinical study, ZM336372 treatment did not lead to inhibition of cell growth in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| BRAF V600E | colon adenocarcinoma | not applicable | N/A | Phase III | Emerging | In a post-hoc analysis of a Phase III trial, BRAF V600E mutations in colon adenocarcinoma patients with microsatellite stable tumors were associated with a shorter disease-free survival and overall survival compared to those patients with microsatellite instability tumors, suggesting that BRAF V600E may serve as a future prognostic biomarker in this patient population (PMID: 26768652). | 26768652 |
| BRAF V600E | hairy cell leukemia | not applicable | N/A | Guideline | Diagnostic | BRAF V600E is diagnostic and aids in distinguishing classic hairy cell leukemia (cHCL) from variant hairy cell leukemia (HCLv) and other B-cell lymphomas and leukemias (PMID: 29118233, NCCN.org). | detail... 29118233 |
| BRAF V600E | melanoma | sensitive | Palbociclib + PD-0325901 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination treatment of PD-0325901 and Ibrance (palbociclib) resulted in significant tumor regression in melanoma cell line xenograft models harboring BRAF V600E and demonstrated a 56% (5/9) complete response rate (PMID: 27488531). | 27488531 |
| BRAF V600E | colorectal carcinoma | no benefit | Palbociclib + PD-0325901 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ibrance (palbociclib) and PD-0325901 demonstrated antagonism in a colorectal carcinoma cell line harboring BRAF V600E in culture (PMID: 37326340). | 37326340 |
| BRAF V600E | colon cancer | sensitive | Cetuximab + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Erbitux (cetuximab) is included in guidelines as primary or subsequent therapy for patients with colon cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | rectum cancer | sensitive | Cetuximab + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Erbitux (cetuximab) is included in guidelines as primary or subsequent therapy for patients with rectal cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | pseudomyxoma peritonei | sensitive | Cetuximab + Encorafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, treatment with the combination of Braftovi (encorafenib) and Erbitux (cetuximab) inhibited viability and induced apoptosis in a patient-derived pseudomyxoma peritonei cell line harboring BRAF V600E in culture and inhibited tumor growth and improved survival of a patient-derived xenograft (PDX) model (PMID: 39018564). | 39018564 |
| BRAF V600E | appendix adenocarcinoma | sensitive | Cetuximab + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Erbitux (cetuximab) is included in guidelines for patients with advanced or metastatic appendiceal adenocarcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | colon neuroendocrine neoplasm | predicted - sensitive | Cetuximab + Encorafenib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Erbitux (cetuximab) and Braftovi (encorafenib) resulted in reduced liver metastasis and a progression-free survival of 14 months in a patient with colorectal neuroendocrine carcinoma harboring BRAF V600E (PMID: 37981300). | 37981300 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Erbitux (cetuximab) is included in guidelines as second-line or subsequent therapy for patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 36307056; ESMO.org). | 36307056 detail... |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | Guideline | Actionable | Braftovi (encorafenib) in combination with Erbitux (cetuximab) is included in the Pan-Asian Guidelines Adaptation (PAGA) as a second- or subsequent-line therapy for patients with advanced or metastatic colorectal cancer harboring BRAF V600E (PMID: 37236086; ESMO.org). | detail... 37236086 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III (BEACON CRC) trial that supported FDA approval, Braftovi (encorafenib) and Erbitux (cetuximab) combination treatment (n=113) resulted in improved median overall survival (8.4 vs 5.4 months, HR=0.60, p<0.001), confirmed response rate (20% vs 2%, p<0.001), and median progression-free survival (4.2 vs 1.5 months, HR=0.40, p<0.001) compared to control (n=107) in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 31566309; NCT02928224). | detail... 31566309 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab) and Encorafenib (LGX818) inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | Clinical Study | Actionable | In a retrospective analysis, real-world treatment with Erbitux (cetuximab) and Braftovi (encorafenib) with or without Mektovi (binimetinib) led to an objective response rate (ORR) of 32.2% (57/201, 2 complete responses (CR)), disease control rate of 71.2% (126/201), median progression-free survival of 4.5 months, and median overall survival of 9.2 months in metastatic colorectal cancer patients with BRAF V600E, with an ORR of 32% (50/180, 1 CR) in patients treated with doublet therapy (PMID: 39255538). | 39255538 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib | Clinical Study | Actionable | In a retrospective study, combination treatment with Erbitux (cetuximab) and Braftovi (encorafenib) resulted in an objective response rate of 17%, a disease control rate of 65%, a median progression-free survival of 4.6 mo, and a median overall survival of 7.2 mo in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 35696748). | 35696748 |
| BRAF V600E | colorectal cancer | sensitive | Alpelisib + Cetuximab + Encorafenib | Phase Ib/II | Actionable | In a Phase Ib/II trial, treatment with the combination of Braftovi (encorafenib), Erbitux (cetuximab), and Piqray (alpelisib) resulted in an overall response rate of 18% (5/28), including 5 patients with a partial response, and led to a median progression free survival of 4.2 months and response duration of 12 weeks in colorectal cancer patients harboring BRAF V600E (PMID: 28363909; NCT01719380). | 28363909 |
| BRAF V600E | colorectal cancer | sensitive | Alpelisib + Cetuximab + Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab), Encorafenib (LGX818) and Alpelisib (BYL719) inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | no benefit | Panitumumab + Trametinib | Phase I | Actionable | In a Phase I trial, combination therapy consisting of Vectibix (panitumumab) and Mekinist (trametinib) resulted in an overall response rate of 0% (0/31), stable disease in 55% (17/31), and a median progression-free survival of 2.6 months in patients with BRAF V600E colorectal cancer (PMID: 29431699; NCT01750918). | 29431699 |
| BRAF V600E | colorectal cancer | predicted - sensitive | Dabrafenib + Panitumumab + Trametinib | Phase I | Actionable | In a Phase I trial, combination therapy consisting of Tafinlar (dabrafenib), Vectibix (panitumumab), and Mekinist (trametinib) resulted in an overall response rate of 21% (19/91, 1 complete response, 18 partial response), stable disease in 65% (59/91), and a median progression-free survival of 4.2 months in patients with BRAF V600E colorectal cancer (PMID: 29431699; NCT01750918). | 29431699 |
| BRAF V600E | melanoma | sensitive | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, RO5126766 (VS-6766) treatment induced cell cycle arrest, decreased Mek and Erk phosphorylation, and inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 25422890). | 25422890 |
| BRAF V600E | melanoma | sensitive | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, RO5126766 inhibited proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 26438159). | 26438159 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | RO5126766 | Preclinical | Actionable | In a preclinical study, RO5126766 inhibited Mek signaling and increased radioiodide uptake and response in transgenic animal models of papillary thyroid carcinoma driven by BRAF V600E (PMID: 27669459). | 27669459 |
| BRAF V600E | colorectal adenocarcinoma | sensitive | RO5126766 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, RO5126766 (VS-6766) inhibited tumor growth in a cell line xenograft model of colorectal adenocarcinoma harboring BRAF V600E (PMID: 23667175). | 23667175 |
| BRAF V600E | melanoma | sensitive | Ravoxertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation in melanoma cell lines harboring BRAF V600E in culture (PMID: 38728872). | 38728872 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | Ravoxertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation in papillary thyroid carcinoma cell lines harboring BRAF V600E in culture (PMID: 38728872). | 38728872 |
| BRAF V600E | colorectal cancer | predicted - sensitive | Ravoxertinib | Case Reports/Case Series | Actionable | In a Phase I trial, two colorectal cancer patients harboring BRAF V600E achieved partial responses lasting 21 and 73 weeks following treatment with Ravoxertinib (GDC-0994) (PMID: 31848189; NCT01875705). | 31848189 |
| BRAF V600E | anaplastic thyroid carcinoma | sensitive | Ravoxertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation and induced cell cycle arrest in an anaplastic thyroid carcinoma cell line harboring BRAF V600E in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 38728872). | 38728872 |
| BRAF V600E | colorectal cancer | no benefit | Cetuximab + Fluorouracil + Irinotecan + Leucovorin + Oxaliplatin | Phase II | Actionable | In a Phase II trial (FIRE-4.5), the combination of Erbitux (cetuximab) with FOLFOXIRI as first-line therapy did not result in an improved objective response rate (ORR) compared to Avastin (bevacizumab) with FOLFOXIRI, with an ORR of 50.8% (30/59) vs 66.7% (20/30) (P=0.92), a median progression-free survival of 7.6 vs 12.4 months (P=0.003), and a median overall survival of 15.2 vs 22.9 months (P=0.14), respectively, in metastatic colorectal cancer patients harboring BRAF V600E (PMID: 37352476). | 37352476 |
| BRAF V600E | melanoma | predicted - sensitive | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 treatment inhibited Erk phosphorylation and reduced growth of melanoma cells harboring BRAF V600E in culture (PMID: 18794803). | 18794803 |
| BRAF V600E | melanoma | sensitive | SCH772984 | Preclinical | Actionable | In a preclinical study, SCH772984 inhibited growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| BRAF V600E | colorectal cancer | sensitive | SCH772984 | Preclinical | Actionable | In a preclinical study, SCH772984 inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| BRAF V600E | melanoma | sensitive | Navitoclax + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX4720 and navitoclax (ABT-263) worked synergistically to inhibit growth and increase apoptosis of BRAF V600E mutant melanoma cells in culture and in xenografts (PMID: 24983357). | 24983357 |
| BRAF V600E | melanoma | sensitive | GSK2126458 + Trametinib | Preclinical | Actionable | In a preclinical study, Mekinist (trametinib) in combination with Omipalisib (GSK2126458) inhibited growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 22389471). | 22389471 |
| BRAF V600E | melanoma | sensitive | CCT196969 | Preclinical - Pdx | Actionable | In a preclinical study, CCT196969 inhibited growth of a human melanoma cell line harboring BRAF V600E in culture, and induced tumor regression in several BRAF V600E-mutant melanoma patient-derived xenograft models (PMID: 25500121). | 25500121 |
| BRAF V600E | melanoma | sensitive | CCT196969 | Preclinical - Cell culture | Actionable | In a preclinical study, CCT196969 treatment inhibited viability of a melanoma cell line harboring BRAF V600E in culture (PMID: 31618628). | 31618628 |
| BRAF V600E | colorectal cancer | sensitive | CCT196969 | Preclinical - Cell culture | Actionable | In a preclinical study, CCT196969 inhibited growth of BRAF-mutant colorectal cancer cell lines in culture (PMID: 25500121), which have been reported to harbor BRAF V600E (PMID: 15294323). | 25500121 15294323 |
| BRAF V600E | melanoma | sensitive | CCT241161 | Preclinical - Pdx | Actionable | In a preclinical study, CCT241161 inhibited growth of a human melanoma cell line harboring BRAF V600E in culture, and induced tumor regression in several BRAF V600E-mutant melanoma patient-derived xenograft models (PMID: 25500121). | 25500121 |
| BRAF V600E | colorectal cancer | sensitive | CCT241161 | Preclinical | Actionable | In a preclinical study, CCT241161 inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 25500121, PMID: 15294323). | 25500121 15294323 |
| BRAF V600E | melanoma | sensitive | S3I-201 | Preclinical | Actionable | In a preclinical study, S3I-201 inhibited cell invasion and Stat3 signaling in human melanoma cell lines harboring BRAF V600E that are resistant to Braf inhibition in culture (PMID: 23242808). | 23242808 |
| BRAF V600E | melanoma | sensitive | Gefitinib + PLX4720 | Preclinical | Actionable | In a preclinical study, Iressa (gefitinib) in combination with PLX4720 inhibited proliferation and tumorigenicity in human melanoma cell line harboring BRAF V600E and resistant to Braf inhibition in culture and in animal models (PMID: 23242808). | 23242808 |
| BRAF V600E | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited growth, downstream MAPK signaling and soft agar growth in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26343583). | 26343583 |
| BRAF V600E | melanoma | sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 treatment inhibited Erk phosphorylation and reduced proliferation of a melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | high grade glioma | predicted - sensitive | LY3009120 | Preclinical - Patient cell culture | Actionable | In a preclinical study, LY3009120 treatment led to inhibition of cell viability and growth in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| BRAF V600E | thyroid cancer | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of thyroid cancer cells harboring BRAF V600E in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring either monomeric BRAF V600E or dimeric isoform of V600E which conferred Zelboraf (vemurafenib)-resistance in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 treatment inhibited Erk phosphorylation and reduced proliferation of a melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | colorectal cancer | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | melanoma | sensitive | SBI-0640756 | Preclinical | Actionable | In a preclinical study, SBI-0640756 inhibited proliferation and Akt/mTOR signaling in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26603897, PMID: 20531415). | 20531415 26603897 |
| BRAF V600E | melanoma | sensitive | SBI-0640726 | Preclinical | Actionable | In a preclinical study, SBI-0640726 inhibited proliferation and Akt/mTOR signaling in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26603897, PMID: 20531415). | 20531415 26603897 |
| BRAF V600E | melanoma | sensitive | BI-69A11 | Preclinical | Actionable | In a preclinical study, BI-69A11 inhibited proliferation and Akt/mTOR signaling in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26603897, PMID: 20531415). | 20531415 26603897 |
| BRAF V600E | melanoma | sensitive | SBI-755199 | Preclinical | Actionable | In a preclinical study, SBI-755199 induced cell death in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26603897). | 26603897 |
| BRAF V600E | melanoma | sensitive | SBI-0640756 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) in combination with SBI-0640756 inhibited the association of eIF4G1 and eIF4E in Zelboraf (vemurafenib) resistant human melanoma cell lines harboring BRAF V600E in culture and reduced tumor growth in xenograft models (PMID: 26603897). | 26603897 |
| BRAF V600E | thyroid cancer | sensitive | CLM3 | Preclinical | Actionable | In a preclinical study, CLM3 inhibited growth, Egfr signaling, and CCND1 expression in thyroid cancer cells harboring BRAF V600E in culture (PMID: 24423321). | 24423321 |
| BRAF V600E | colon cancer | sensitive | Navitoclax + Vemurafenib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Zelboraf (vemurafenib) on human colon cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | sensitive | Navitoclax + Vemurafenib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Zelboraf (vemurafenib) on human melanoma cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Navitoclax + Vemurafenib | Preclinical | Actionable | In a preclinical study, Navitoclax (ABT-263) enhanced the inhibitory effect of Zelboraf (vemurafenib) on human non-small cell lung cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | sensitive | TW-37 + Vemurafenib | Preclinical | Actionable | In a preclinical study, TW-37 enhanced the inhibitory effect of Zelboraf (vemurafenib) on human melanoma cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | TW-37 + Vemurafenib | Preclinical | Actionable | In a preclinical study, TW-37 enhanced the inhibitory effect of Zelboraf (vemurafenib) on human non-small cell lung cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | sensitive | Trametinib + TW-37 | Preclinical | Actionable | In a preclinical study, TW-37 enhanced the inhibitory effect of Mekinist (trametinib) on human melanoma cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | lung non-small cell carcinoma | sensitive | Trametinib + TW-37 | Preclinical | Actionable | In a preclinical study, TW-37 enhanced the inhibitory effect of Mekinist (trametinib) on human non-small cell lung cancer cells harboring BRAF V600E in culture (PMID: 25665005). | 25665005 |
| BRAF V600E | melanoma | sensitive | Cediranib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX4720 and Cediranib (AZD-2171) worked synergistically to inhibit cell growth and induce apoptosis in PLX4720-resistant human melanoma cell lines harboring BRAF V600E in culture and to suppress tumor growth in xenograft models (PMID: 26461489). | 26461489 |
| BRAF V600E | melanoma | sensitive | Cediranib + PLX4720 + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, PLX4720, Cediranib (AZD-2171) and Koselugo (selumetinib) worked synergistically to inhibit cell growth in PLX4720-resistant melanoma cell lines harboring BRAF V600E in culture (PMID: 26461489). | 26461489 |
| BRAF V600E | melanoma | sensitive | PLX4720 + Tivozanib | Preclinical | Actionable | In a preclinical study, PLX4720 and Tivozanib (AV-951) worked synergistically to inhibit cell growth in PLX4720-resistant melanoma cell lines harboring BRAF V600E in culture (PMID: 26461489). | 26461489 |
| BRAF V600E | melanoma | sensitive | BI 882370 + Trametinib | Preclinical | Actionable | In a preclinical study, xenograft models of melanoma harboring BRAF V600E treated with the combination of BI 882370 and Mekinist (trametinib) demonstrated tumor regression with no regrowth during the 5 weeks of treatment (PMID: 26916115). | 26916115 |
| BRAF V600E | colorectal cancer | sensitive | BI 882370 + Trametinib | Preclinical | Actionable | In a preclinical study, colorectal cancer cells harboring BRAF V600E were sensitive to the combination of BI 882370 and Mekinist (trametinib) in xenograft models, resulting in tumor growth inhibition and partial tumor regression (PMID: 26916115). | 26916115 |
| BRAF V600E | colorectal cancer | sensitive | BI 882370 + Cetuximab | Preclinical | Actionable | In a preclinical study, colorectal cancer cells harboring BRAF V600E were sensitive to the combination of BI 882370 and Erbitux (cetuximab) in xenograft models, resulting in tumor growth inhibition and partial tumor regression (PMID: 26916115). | 26916115 |
| BRAF V600E | colorectal cancer | sensitive | Afatinib + BI 882370 | Preclinical | Actionable | In a preclinical study, colorectal cancer cells harboring BRAF V600E were sensitive to the combination of BI 882370 and Gilotrif (afatinib) in xenograft models, resulting in tumor growth inhibition and partial tumor regression (PMID: 26916115). | 26916115 |
| BRAF V600E | melanoma | sensitive | DEL-22379 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, DEL-22379 inhibited growth of melanoma cells harboring BRAF V600E with high levels of ERK dimerization in culture and inhibited tumor progression in melanoma xenograft models harboring BRAF V600E (PMID: 26267534). | 26267534 |
| BRAF V600E | colorectal adenocarcinoma | sensitive | DEL-22379 | Preclinical - Pdx | Actionable | In a preclinical study, DEL-22379 inhibited tumor growth in a colorectal adenocarcinoma patient-derived xenograft model harboring BRAF V600E (PMID: 26267534). | 26267534 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + GSK2126458 | Preclinical | Actionable | In a preclinical study, Tafinlar (dabrafenib) in combination with Omipalisib (GSK2126458) resulted in improved growth inhibition of human melanoma cell lines harboring BRAF V600E in culture (PMID: 22389471). | 22389471 |
| BRAF V600E | thyroid cancer | predicted - sensitive | Lifirafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Lifirafenib (BGB-283) treatment resulted in partial response in 15.1% (8/53) of solid tumor patients with BRAF mutations, including 2 thyroid cancer patients harboring BRAF V600E (1 in dose-escalation phase, 1 in the dose-expansion), and in the dose-expansion phase 1 of 3 thyroid cancer patients harboring a BRAF V600 mutation demonstrated a partial response and 2 demonstrated stable disease, resulting in a disease control rate of 100% (3/3) (PMID: 32182156; NCT02610361). | 32182156 |
| BRAF V600E | melanoma | sensitive | Lifirafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Lifirafenib (BGB-283) inhibited Braf phosphorylation and cell proliferation in melanoma cell lines harboring BRAF V600E in culture (PMID: 26208524). | 26208524 |
| BRAF V600E | melanoma | sensitive | Lifirafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Lifirafenib (BGB-283) treatment inhibited viability of a melanoma cell line harboring BRAF V600E in culture (PMID: 31618628). | 31618628 |
| BRAF V600E | colorectal cancer | sensitive | Lifirafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Lifirafenib (BGB-283) inhibited Braf phosphorylation and cell proliferation in colorectal cancer cell lines harboring BRAF V600E in culture, and resulted in partial tumor regression in both cell line and patient-derived xenograft models (PMID: 26208524). | 26208524 |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | Lifirafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Lifirafenib (BGB-283) treatment demonstrated safety and resulted in partial response (PR) in 15.1% (8/53) of advanced solid tumor patients harboring a BRAF mutation, including 1 patient with BRAF V600E-mutant low-grade serous ovarian cancer (PMID: 32182156; NCT02610361). | 32182156 |
| BRAF V600E | Advanced Solid Tumor | sensitive | Lifirafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Lifirafenib (BGB-283) inhibited viability of a variety of cancer cell lines harboring BRAF V600E in culture (PMID: 26208524). | 26208524 |
| BRAF V600E | colorectal carcinoma | sensitive | Gedatolisib + Palbociclib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ibrance (palbociclib) and Gedatolisib (PF-05212384) synergistically inhibited growth of a colorectal carcinoma cell line harboring BRAF V600E in culture (PMID: 37326340). | 37326340 |
| BRAF V600E | colorectal cancer | sensitive | DT01 + Fluorouracil + Oxaliplatin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, DT01 increased sensitivity of human colorectal cancer (CRC) cells harboring BRAF V600E to Eloxatin (oxaliplatin) and Adrucil (5-fluorouracil), and the combination resulted in decreased liver tumor growth in CRC cell line xenograft metastasis models (PMID: 26637369). | 26637369 |
| BRAF V600E | melanoma | sensitive | DETD-35 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, DETD-35 inhibited proliferation and colony formation of melanoma cells harboring BRAF V600E in culture and reduced tumor size in xenograft models (PMID: 27048951). | 27048951 |
| BRAF V600E | melanoma | sensitive | DETD-35 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, DETD-35 and Zelboraf (vemurafenib) synergistically inhibited proliferation and colony formation of melanoma cells harboring BRAF V600E in culture and reduced tumor size in xenograft models (PMID: 27048951). | 27048951 |
| BRAF V600E | neuroendocrine tumor | predicted - sensitive | Trametinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) and Zelboraf (vemurafenib) combination treatment resulted in a rapid and sustained clinical response in a patient with a rectal neuroendocrine tumor harboring a BRAF V600E mutation (PMID: 27048246). | 27048246 |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Trametinib + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) and Mekinist (trametinib) combination treatment resulted in decreased tumor markers in a patient with pancreatic ductal adenocarcinoma harboring BRAF V600E, as well as a germline ATM mutation, and the patient received 13 months of combination therapy and was followed for 24 months (PMID: 35145907). | 35145907 |
| BRAF V600E | melanoma | sensitive | SB590885 | Preclinical - Cell culture | Actionable | In a preclinical study, SB590885 inhibited proliferation of melanoma cell lines harboring either monomeric BRAF V600E or dimeric isoform of V600E which conferred Zelboraf (vemurafenib)-resistance in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | Advanced Solid Tumor | sensitive | SB590885 | Preclinical | Actionable | In a preclinical study, SB590885 inhibited inhibited Erk phosphorylation and cell proliferation of transformed cells expression BRAF V600E in culture (PMID: 20538618). | 20538618 |
| BRAF V600E | melanoma | predicted - sensitive | LXH 254 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E was sensitive to treatment with LXH254, demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth and tumor regression in a cell line xenograft model of melanoma (PMID: 33355204). | 33355204 |
| BRAF V600E | melanoma | no benefit | SHP099 | Preclinical | Actionable | In a preclinical study, SHP099 did not inhibit proliferation or ERK activation in a melanoma cell line harboring BRAF V600E in culture (PMID: 27362227). | 27362227 |
| BRAF V600E | colorectal cancer | resistant | SHP099 | Preclinical - Cell culture | Actionable | In a preclincial study, colorectal cancer cell lines harboring BRAF V600E demonstrated resistance to SHP099 in culture (PMID: 27362227). | 27362227 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Dabrafenib | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab) and Tafinlar (dabrafenib) inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Koselugo (selumetinib) and Erbitux (cetuximab) combination treatment inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colon adenocarcinoma | predicted - sensitive | Cetuximab + Dabrafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, the combination of Tafinlar (dabrafenib), Mekinist (trametinib), and Erbitux (cetuximab) resulted in a partial response after 2 months followed by a complete response in a patient with microsatellite-stable, metastatic colon adenocarcinoma harboring BRAF V600E, and the patient remained in complete remission 11 months after discontinuation of treatment (PMID: 37213293). | 37213293 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Dabrafenib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab), Tafinlar (dabrafenib), and Mekinist (trametinib) inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Dabrafenib + SCH772984 | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab), Tafinlar (dabrafenib), and SCH772984 inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + SCH772984 | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Erbitux (cetuximab) and SCH772984 inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | thyroid cancer | sensitive | Dabrafenib + SCH772984 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Tafinlar (dabrafenib) and SCH772984 synergistically inhibited cell growth of thyroid cancer cell lines harboring BRAF V600E in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 33595872). | 33595872 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + SCH772984 | Preclinical - Cell culture | Actionable | In a preclinical study, combination therapy consisting of Tafinlar (dabrafenib) and SCH772984 inhibited survival of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 27312529). | 27312529 |
| BRAF V600E | melanoma | sensitive | LY3214996 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, LY3214996 treatment in a melanoma cell line harboring BRAF V600E led to decreased cell proliferation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 31744895). | 31744895 |
| BRAF V600E | colorectal cancer | predicted - sensitive | LY3214996 | Preclinical - Cell culture | Actionable | In a preclinical study, a lung cancer cell line harboring BRAF V600E and NF1 T2805I was sensitive to treatment with LY3214996 in culture, demonstrating decreased cell viability (PMID: 31744895). | 31744895 |
| BRAF V600E | thyroid cancer | sensitive | Dasatinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Sprycel (dasatinib) and Mekinist (trametinib) synergistically inhibited proliferation and induced apoptosis in both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| BRAF V600E | thyroid cancer | sensitive | Dasatinib + Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Sprycel (dasatinib) and Koselugo (selumetinib) synergistically inhibited proliferation and induced apoptosis in both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| BRAF V600E | thyroid cancer | sensitive | Dasatinib + SCH772984 | Preclinical - Cell culture | Actionable | In a preclinical study, Sprycel (dasatinib) and SCH772984 synergistically inhibited proliferation and induced apoptosis in both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). | 27222538 |
| BRAF V600E | melanoma | sensitive | PAC-1 + Trametinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of PAC-1 to Mekinist (trametinib) and Zelboraf (vemurafenib) led to greater levels of caspase-3 activity and apoptosis in melanoma cells harboring BRAF V600E when compared to Zelboraf (vemurafenib) and Mekinist (trametinib) treatment without PAC-1 (PMID: 27297867). | 27297867 |
| BRAF V600E | melanoma | sensitive | PAC-1 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PAC-1 and Zelboraf (vemurafenib) resulted in a synergistic effect when treating melanoma cells harboring BRAF V600E in culture and xenograft models, demonstrating increased apoptosis and decreased tumor volume (PMID: 27297867). | 27297867 |
| BRAF V600E | melanoma | sensitive | PLX7904 | Preclinical - Cell culture | Actionable | In a preclinical study, PLX7904 inhibited survival of melanoma cell lines harboring monomeric BRAF V600E as well as cells harboring the Zelboraf (vemurafenib)-resistant dimeric BRAF V600E in culture (PMID: 26466569). | 26466569 |
| BRAF V600E | colorectal cancer | sensitive | PLX7904 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX7904 inhibited survival of colorectal cancer cells harboring BRAF V600E in culture and demonstrated anti-tumor activity in cell line xenograft models (PMID: 26466569). | 26466569 |
| BRAF V600E | colorectal cancer | sensitive | PLX4720 + TAK-632 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PLX4720 and TAK-632 combination treatment resulted in durable inhibition of Erk signaling and tumor growth in xenograft models of colorectal cancer cells harboring BRAF V600E (PMID: 27523909). | 27523909 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Lifirafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lifirafenib (BGB-283) in combination with Erbitux (cetuximab) demonstrated enhanced tumor suppression in colorectal cancer cell line xenograft models harboring BRAF V600E (PMID: 26208524). | 26208524 |
| BRAF V600E | colorectal cancer | sensitive | Everolimus + Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 23629727). | 23629727 |
| BRAF V600E | colorectal cancer | sensitive | Pimasertib + Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 23629727). | 23629727 |
| BRAF V600E | skin melanoma | predicted - sensitive | Dabrafenib + Nivolumab + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mekinist (trametinib), Tafinlar (dabrafenib), and Opdivo (nivolumab) resulted in a partial response in the leptomeningeal disease on the spine and the extracranial melanoma, with the intracranial lesions remaining stable after 6 months, in a patient with cutaneous melanoma harboring BRAF V600E, and a follow-up at least 7 years following diagnosis demonstrated complete remission (PMID: 38960393). | 38960393 |
| BRAF V600E | skin melanoma | sensitive | Atezolizumab + Cobimetinib + Vemurafenib | Guideline | Actionable | Zelboraf (vemurafenib) plus Cotellic (cobimetinib) in combination with an immune checkpoint inhibitor, such as Tecentriq (atezolizumab), is included in guidelines as second-line or subsequent therapy (category 2A) for patients with metastatic or unresectable cutaneous melanoma harboring a BRAF V600 mutation, such as BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Binimetinib + Cetuximab + Encorafenib | Case Reports/Case Series | Actionable | In a clinical case study, third-line treatment with the combination of Mektovi (binimetinib), Erbitux (cetuximab), and Braftovi (encorafenib) resulted in a partial response with a 74% decrease in primary tumor size in a patient with metastatic pancreatic ductal adenocarcinoma harboring BRAF V600E (PMID: 39461261). | 39461261 |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Cetuximab + Encorafenib | Phase II | Actionable | In a Phase II (ANCHOR CRC) trial, Braftovi (encorafenib), Mektovi (binimetinib), and Erbitux (cetuximab) combination treatment (n=95) demonstrated an acceptable safety profile and resulted in a confirmed objective response rate of 47.8% (44/92), a disease control rate of 88% (81/92), a median progression-free survival of 5.8 months, and a median overall survival of 18.3 months in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 36763936; NCT03693170). | 36763936 |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Cetuximab + Encorafenib | Phase III | Actionable | In a Phase III (BEACON CRC) trial, Braftovi (encorafenib), Mektovi (binimetinib), and Erbitux (cetuximab) combination treatment (n=111) resulted in improved median overall survival (9.0 vs 5.4 months, HR=0.52, p<0.001), confirmed response rate (26% vs 2%, p<0.001), and median progression-free survival (4.3 vs 1.5 months, HR=0.38, p<0.001) compared to control (n=107) in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 31566309; NCT02928224). | 31566309 |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Cetuximab + Encorafenib | Clinical Study | Actionable | In a retrospective analysis, real-world treatment with Erbitux (cetuximab) and Braftovi (encorafenib) with or without Mektovi (binimetinib) led to an objective response rate (ORR) of 32.2% (57/201, 2 complete responses (CR)), disease control rate of 71.2% (126/201), median progression-free survival of 4.5 months, and median overall survival of 9.2 months in metastatic colorectal cancer patients with BRAF V600E, with an ORR of 33.3% (7/21, 1 CR) in patients treated with triplet therapy (PMID: 39255538). | 39255538 |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Cetuximab + Encorafenib | Clinical Study | Actionable | In a retrospective study, combination treatment with Mektovi (binimetinib), Erbitux (cetuximab), and Braftovi (encorafenib) resulted in an objective response rate of 31%, a disease control rate of 78%, a median progression-free survival of 4.2 mo, and a median overall survival of 7.1 mo in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 35696748). | 35696748 |
| BRAF V600E | high grade glioma | predicted - sensitive | Everolimus + Selumetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Selumetinib (AZD6244) and Afinitor (everolimus) synergistically inhibited growth and induced apoptosis in glioma cell lines in culture, resulted in prolonged survival in cell line xenograft models (PMID: 27217440). | 27217440 |
| BRAF V600E | high grade glioma | predicted - sensitive | Everolimus + PLX4720 | Preclinical - Cell culture | Actionable | In a preclinical study, Afinitor (everolimus) and PLX4720 synergistically inhibited growth and induced apoptosis in glioma cell lines in culture (PMID: 27217440). | 27217440 |
| BRAF V600E | melanoma | sensitive | Imatinib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Gleevec (imatinib) and PLX4720 enhanced antitumor efficacy of melanoma cells harboring BRAF V600E, demonstrating decreased cell survival in xenograft models, and decreased phosphorylation of Mapk1 in culture (PMID: 27924459). | 27924459 |
| BRAF V600E | melanoma | sensitive | Alpelisib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Alpelisib (BYL719) and PLX4720 enhanced antitumor activity in a melanoma cell line harboring BRAF V600E, demonstrating decreased cell survival and increased apoptotic activity in xenograft models, and decreased Akt signaling in culture (PMID: 27924459). | 27924459 |
| BRAF V600E | melanoma | sensitive | Erlotinib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720 and Tarceva (erlotinib) resulted in antitumor efficacy in a melanoma cell line harboring BRAF V600E, demonstrating decreased cell survival and increased apoptotic activity in xenograft models and culture (PMID: 27924459). | 27924459 |
| BRAF V600E | melanoma | sensitive | PLX4720 + Vorinostat | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720 and Zolinza (vorinostat) resulted in antitumor efficacy in a melanoma cell line harboring BRAF V600E, demonstrating decreased cell survival and increased apoptotic activity in xenograft models, and decreased Rb phosphorylation in culture (PMID: 27924459). | 27924459 |
| BRAF V600E | melanoma | sensitive | Doxorubicin + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720 and Adriamycin (doxorubicin) resulted in antitumor efficacy in a melanoma cell line harboring BRAF V600E, demonstrating decreased cell survival and increased apoptotic activity in xenograft models, and inhibition of cell growth in culture (PMID: 27924459). | 27924459 |
| BRAF V600E | glioblastoma | sensitive | BI2536 + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of BI 2536 and PLX4720 resulted in suppression of downstream signaling, increased apoptotic activity, inhibition of cell proliferation, and tumor growth suppression in glioblastoma cell line xenograft models harboring BRAF V600E (PMID: 26573800). | 26573800 |
| BRAF V600E | Advanced Solid Tumor | predicted - sensitive | PF-00477736 + PF3644022 | Preclinical - Cell culture | Actionable | In a preclinical study, Chk1 inhibitor PF-477736 and MK2 inhibitor PF3644022 synergistically inhibited growth of transformed cells over expressing BRAF V600E in culture, while single agent inhibition had no effect (PMID: 26140595). | 26140595 |
| BRAF V600E | melanoma | sensitive | ASN003 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma xenograft model harboring BRAF V600E demonstrated tumor regression when treated with ASN003 (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr B100). | detail... |
| BRAF V600E | melanoma | decreased response | Toripalimab-tpzi | Clinical Study | Actionable | In a retrospective analysis, real-world treatment with either Keytruda (pembrolizumab) or Loqtorz (toripalimab-tpzi) resulted in a median disease-free survival of 17 months in melanoma patients harboring BRAF V600E compared to 32 months in patients with wild-type BRAF, NRAS, and KIT (p=0.022) (PMID: 37403699). | 37403699 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Spartalizumab + Trametinib | Phase II | Actionable | In a Phase II trial, the combination of Spartalizumab (PDR001), Tafinlar (dabrafenib), and Mekinist (trametinib) was well tolerated and resulted in a confirmed objective response rate of 24.3% (9/37, 2 complete responses), disease control rate of 70.3% (26/37), median progression-free survival of 4.3 months, median duration of response of 7.4 months, and median overall survival of 13.6 months in patients with metastatic colorectal cancer harboring BRAF V600E (PMID: 36702949; NCT03668431). | 36702949 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720 and Erbitux (cetuximab) inhibited tumor growth in colorectal cancer cell line xenograft models harboring BRAF V600E (PMID: 22281684). | 22281684 |
| BRAF V600E | colon cancer | predicted - sensitive | Cetuximab + Sorafenib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic colon cancer harboring BRAF V600E demonstrated mixed radiographic response with slight progression in some locations and stable disease in other locations for 7 months following treatment with the combination of Nexavar (sorafenib) and Erbitux (cetuximab) (PMID: 23792568). | 23792568 |
| BRAF V600E | melanoma | sensitive | INU-152 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, INU-152 reduced MEK and ERK phosphorylation and growth of a melanona cell line harboring BRAF V600E in culture, and inhibited tumor growth in xenograft models (PMID: 28645859). | 28645859 |
| BRAF V600E | colorectal cancer | sensitive | INU-152 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, INU-152 inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture, and reduced tumor growth in BRAF V600E-mutant colorectal cancer cell line xenograft models (PMID: 28645859). | 28645859 |
| BRAF V600E | melanoma | sensitive | BGB659 | Preclinical - Cell culture | Actionable | In a preclinical study, BGB659 treatment inhibited Erk phosphorylation and reduced proliferation of a melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | colorectal cancer | predicted - sensitive | LSN3074753 | Preclinical - Pdx | Actionable | In a preclinical study, LSN3074753 demonstrated modest efficacy in patient-derived xenograft models of colorectal cancer harboring BRAF V600E, resulted in tumor growth inhibition or regression, but relapse upon discontinuation of treatment (PMID: 28611205). | 28611205 |
| BRAF V600E | melanoma | sensitive | EBI-907 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, EBI-907 inhibited BRAF and ERK signaling, resulted in growth inhibition of melanoma cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 26810733). | 26810733 |
| BRAF V600E | colorectal cancer | sensitive | EBI-907 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, EBI-907 inhibited BRAF and ERK signaling, resulted in growth inhibition of colorectal cancer cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 26810733). | 26810733 |
| BRAF V600E | melanoma | decreased response | Dabrafenib + SCH772984 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination of Tafinlar (dabrafenib), SCH772984, and Mekinist (trametinib) resulted in durable inhibition of Erk signaling and proliferation of melanoma cells overexpressing BRAF V600E in culture (PMID: 28714990). | 28714990 |
| BRAF V600E | lung non-small cell carcinoma | predicted - sensitive | LTT462 + LXH 254 | Case Reports/Case Series | Actionable | In a Phase Ib trial, LTT462 and LXH 254 combination therapy was well tolerated and resulted in an unconfirmed partial response (PR) in 4% (2/49) and stable disease (SD) in 33% (16/49) of patients with advanced or metastatic KRAS- or BRAF-mutant non-small cell lung cancer, with 1 patient harboring BRAF V600E achieving an unconfirmed PR and 1 achieving SD with over 25% tumor reduction (Ann Oncol 31 (suppl 4):S881-S882; NCT02974725). | detail... |
| BRAF V600E | melanoma | sensitive | ASTX029 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ASTX029 treatment reduced Erk and Rsk phosphorylation, induced cell-cycle arrest, and inhibited growth of a melanoma cell line harboring BRAF V600E in culture and inhibited tumor growth in cell line xenograft models, and was also effective against cells with acquired resistance to Zelboraf (vemurafenib) or Koselugo (selumetinib) (PMID: 34330842). | 34330842 |
| BRAF V600E | colorectal adenocarcinoma | sensitive | ASTX029 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ASTX029 treatment reduced Erk and Rsk phosphorylation and inhibited growth of colorectal adenocarcinoma cell lines harboring BRAF V600E in culture, and inhibited tumor growth and induced tumor regression in cell line xenograft models (PMID: 34330842). | 34330842 |
| BRAF V600E | melanoma | sensitive | RAF709 | Preclinical - Cell culture | Actionable | In a preclinical study, RAF709 inhibited Erk signaling and proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 29343524). | 29343524 |
| BRAF V600E | melanoma | predicted - sensitive | Belvarafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Belvarafenib (HM95573) treatment led to inhibition of tumor growth in a melanoma cell line xenograft model harboring BRAF V600E (PMID: 33953400). | 33953400 |
| BRAF V600E | high grade glioma | predicted - sensitive | Belvarafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Belvarafenib (HM95573) treatment led to inhibition of cell viability in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| BRAF V600E | colorectal cancer | predicted - sensitive | Belvarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Belvarafenib (HM95573) treatment in a colorectal cancer patient harboring BRAF V600E led to a tumor reduction of 39% after 8 weeks of treatment and a confirmed partial response at 12 weeks, and response to treatment was maintained for 8 weeks (PMID: 33953400; NCT03118817). | 33953400 |
| BRAF V600E | melanoma | predicted - sensitive | BGB3245 | Case Reports/Case Series | Actionable | In a Phase I trial, BGB3245 treatment demonstrated manageable safety and resulted in a disease control rate of 48% (16/33,1 complete response, 5 confirmed partial responses (PR), 2 unconfirmed PR, and 8 stable disease > 24 weeks) in patients with advanced solid tumors harboring MAPK pathway alterations, including 1 complete response and 1 confirmed partial response in patients with melanoma harboring BRAF V600E (Cancer Res (2023) 83 (8_Supplement): CT031). | detail... |
| BRAF V600E | cholangiocarcinoma | predicted - sensitive | BGB3245 | Case Reports/Case Series | Actionable | In a Phase I trial, BGB3245 treatment demonstrated manageable safety and resulted in a disease control rate of 48% (16/33,1 complete response, 5 confirmed partial responses (PR), 2 unconfirmed PR, and 8 stable disease > 24 weeks) in patients with advanced solid tumors harboring MAPK pathway alterations, including a partial response in a patient with cholangiocarcinoma harboring BRAF V600E (Cancer Res (2023) 83 (8_Supplement): CT031). | detail... |
| BRAF V600E | ovarian serous carcinoma | predicted - sensitive | BGB3245 | Case Reports/Case Series | Actionable | In a Phase I trial, BGB3245 treatment demonstrated manageable safety and resulted in a disease control rate of 48% (16/33,1 complete response, 5 confirmed partial responses (PR), 2 unconfirmed PR, and 8 stable disease > 24 weeks) in patients with advanced solid tumors harboring MAPK pathway alterations, including a partial response in a patient with low grade serous ovarian carcinoma harboring BRAF V600E (Cancer Res (2023) 83 (8_Supplement): CT031). | detail... |
| BRAF V600E | melanoma | resistant | RMC-4550 | Preclinical - Cell culture | Actionable | In a preclinical study, RMC-4550 did not inhibit Erk phosphorylation or proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 30104724). | 30104724 |
| BRAF V600E | melanoma | sensitive | ERAS-007 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, ERAS-007 (ASN007) treatment inhibited proliferation and Erk signaling in a melanoma cell line harboring BRAF V600E in culture, and inhibited tumor growth in patient-derived xenograft (PDX) models, including a Zelboraf (vemurafenib)-resistant PDX model (PMID: 34337566). | 34337566 |
| BRAF V600E | colorectal cancer | sensitive | ERAS-007 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, ERAS-007 (ASN007) treatment inhibited cell proliferation and Erk signaling in colorectal cancer cell lines harboring BRAF V600E in culture, and induced tumor regression in two patient-derived xenograft (PDX) models (PMID: 34337566). | 34337566 |
| BRAF V600E | diffuse large B-cell lymphoma | sensitive | ERAS-007 | Preclinical - Cell culture | Actionable | In a preclinical study, ERAS-007 (ASN007) treatment inhibited proliferation of diffuse large B-cell lymphoma cells harboring BRAF V600E in culture (PMID: 34337566). | 34337566 |
| BRAF V600E | Cancer of Unknown Primary | predicted - sensitive | Binimetinib + Cetuximab | Case Reports/Case Series | Actionable | In a clinical case study, treatment with the combination of Mektovi (binimetinib) and Erbitux (cetuximab) resulted in a significant but brief response in all lesions in a patient with metastatic cancer of unknown primary harboring BRAF V600E (PMID: 39391046). | 39391046 |
| BRAF V600E | melanoma | predicted - resistant | BI-3406 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, BI-3406 treatment failed to inhibit growth of KRAS wild-type melanoma cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 32816843). | 32816843 |
| BRAF V600E | colorectal cancer | predicted - resistant | BI-3406 | Preclinical - Cell culture | Actionable | In a preclinical study, BI-3406 treatment failed to inhibit growth of colorectal cancer cells harboring BRAF V600E in culture (PMID: 32816843). | 32816843 |
| BRAF V600E | colorectal cancer | sensitive | Tazemetostat + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Tazverik (tazemetostat) sensitized a colorectal cancer cell line harboring BRAF V600E to Mekinist (trametinib) treatment in culture, resulting in decreased cell proliferation (PMID: 39121480). | 39121480 |
| BRAF V600E | colon cancer | sensitive | Encorafenib + Panitumumab | Guideline | Actionable | Braftovi (encorafenib) in combination with Vectibix (panitumumab) is included in guidelines as primary or subsequent therapy for patients with colon cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | rectum cancer | sensitive | Encorafenib + Panitumumab | Guideline | Actionable | Braftovi (encorafenib) in combination with Vectibix (panitumumab) is included in guidelines as primary or subsequent therapy for patients with rectal cancer harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | appendix adenocarcinoma | sensitive | Encorafenib + Panitumumab | Guideline | Actionable | Braftovi (encorafenib) in combination with Vectibix (panitumumab) is included in guidelines for patients with advanced or metastatic appendiceal adenocarcinoma harboring BRAF V600E (NCCN.org). | detail... |
| BRAF V600E | melanoma | sensitive | Tunlametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Tunlametinib (HL-085) inhibited viability and induced cell cycle arrest in melanoma cell lines harboring BRAF V600E in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37808191). | 37808191 |
| BRAF V600E | colorectal cancer | sensitive | Tunlametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Tunlametinib (HL-085) inhibited viability of a colorectal cancer cell line harboring BRAF V600E in culture and inhibited tumor growth in a cell line xenograft model (PMID: 37808191). | 37808191 |
| BRAF V600E | melanoma | predicted - sensitive | JSI-1187 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, JSI-1187 treatment in a melanoma cell line harboring BRAF V600E led to inhibition of cell proliferation in culture, and tumor growth inhibition in a cell line xenograft model (Cancer Res 2020;80(16 Suppl):Abstract nr 4188). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | JSI-1187 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, JSI-1187 treatment in a colorectal cancer cell line harboring BRAF V600E led to inhibition of cell proliferation in culture, and tumor regression and dose-dependent tumor growth inhibition in a cell line xenograft model (Cancer Res 2020;80(16 Suppl):Abstract nr 4188). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | Dabrafenib + JSI-1187 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Tafinlar (dabrafenib) and JSI-1187 led to synergistic inhibition of tumor growth in a colorectal cancer cell line xenograft model harboring BRAF V600E (Cancer Res 2020;80(16 Suppl):Abstract nr 4188). | detail... |
| BRAF V600E | thyroid cancer | sensitive | PLX4720 + Ponatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Iclusig (ponatinib) and PLX4720 treatment demonstrated synergy, and inhibited Erk, Mek, and c-jun phosphorylation, reduced cell proliferation, colony formation, and migration, and induced apoptosis in thyroid cancer cells harboring BRAF V600E and in PLX4720-resistant cells harboring BRAF V600E in culture, and inhibited tumor growth, reduced lung and liver metastases, and increased survival in cell line xenograft models (PMID: 31937621). | 31937621 |
| BRAF V600E | thyroid cancer | sensitive | Ponatinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) and Zelboraf (vemurafenib) treatment synergistically inhibited proliferation of thyroid cancer cells harboring BRAF V600E in culture (PMID: 31937621). | 31937621 |
| BRAF V600E | melanoma | no benefit | Cobimetinib + Pembrolizumab + Vemurafenib | Phase I | Actionable | In a Phase I trial, combination of Cotellic (cobimetinib), Zelboraf (vemurafenib), and Keytruda (pembrolizumab) resulted in unreached median progression-free survival and overall survival in patients with advanced melanoma harboring BRAF V600E or V600K mutations, however, the trial was closed due to high incidence of dose-limiting toxicity and decreased health utility at 1 year (J Clin Oncol 39, no. 15_suppl, abstract e21506; NCT02818023). | detail... |
| BRAF V600E | lung non-small cell carcinoma | unknown | unspecified immune checkpoint inhibitor | Clinical Study - Cohort | Actionable | In a retrospective clinical study, patients with non-small cell lung cancer harboring rare targetable drivers (RTD) (BRAF, ERBB2/3, RET, MET, ROS1, NTRK) who received immune checkpoint inhibitors (ICI) achieved longer median overall survival (mOS) (32 vs 13 mo, p=0.01) compared to those who did not receive ICI, mOS was not reached in patients harboring BRAF V600E (n=5) mutations, although RTD type was not associated with OS in a univariate analysis (PMID: 30268448). | 30268448 |
| BRAF V600E | colorectal cancer | decreased response | unspecified immune checkpoint inhibitor | Clinical Study - Cohort | Actionable | In a retrospective analysis, treatment with Keytruda (pembrolizumab), Opdivo (nivolumab), or combination treatment with Opdivo (nivolumab) and Yervoy (ipilimumab) in patients with mismatch repair-deficient colorectal cancer harboring BRAF V600E vs. patients with wild-type BRAF resulted in a lower objective response rate (44.4% vs. 74.2%, p = 0.12) and shorter progression-free survival (PFS) rates (1-year PFS 40% vs. 73.3%, 2-year PFS 26.7% vs. 73.3%) (PMID: 33631043). | 33631043 |
| BRAF V600E | thyroid cancer | sensitive | SHP099 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and SHP099 inhibited proliferation and induced cell cycle arrest in Zelboraf (vemurafenib)-resistant thyroid cancer cell lines harboring BRAF V600E in culture and inhibited tumor growth in a cell line xenograft model (PMID: 37325052). | 37325052 |
| BRAF V600E | lung non-small cell carcinoma | predicted - sensitive | Lifirafenib + PD-0325901 | Phase I | Actionable | In a Phase Ib trial, Lifirafenib (BGB-283) and PD-0325901 combination treatment demonstrated safety and activity in patients with advanced solid tumors harboring MAPK pathway alterations, resulting in an objective response rate of 27.8% (15/54, 1 complete and 14 partial responses), including an objective response in a patient with non-small cell lung cancer harboring BRAF V600E (Cancer Res (2023) 83 (8_Supplement): CT033). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Capecitabine + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with Xeloda (capecitabine) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 22180495). | 22180495 |
| BRAF V600E | colorectal cancer | sensitive | Bevacizumab + Capecitabine + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment when combined with Xeloda (capecitabine) and Avastin (bevacizumab) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 22180495). | 22180495 |
| BRAF V600E | colorectal cancer | sensitive | Irinotecan + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with Camptosar (irinotecan) enhanced tumor growth inhibition and increased survival in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 22180495). | 22180495 |
| BRAF V600E | melanoma | sensitive | C6-ceramide nanoliposome + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Nexavar (sorafenib) treatment in combination with C6-ceramide nanoliposome inhibited Mek and Akt phosphorylation, led to enhanced apoptosis and inhibition of proliferation, and synergistically reduced viability of melanoma cells harboring BRAF V600E in culture, and enhanced inhibition of tumor growth in a cell line xenograft model (PMID: 18519791). | 18519791 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib + Fluorouracil + Irinotecan + Leucovorin | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Erbitux (cetuximab), Braftovi (encorafenib), and FOLFIRI resulted in increased tumor growth inhibition and tumor regression compared to Erbitux (cetuximab) plus Braftovi (encorafenib) or FOLFIRI alone in patient-derived xenograft (PDX) models of colorectal cancer harboring BRAF V600E and increased survival and tumor growth inhibition in cell line xenograft models (PMID: 37040395). | 37040395 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib + Fluorouracil + Leucovorin + Oxaliplatin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of Erbitux (cetuximab), Braftovi (encorafenib), and FOLFOX resulted in increased tumor growth inhibition and survival compared to Erbitux (cetuximab) plus Braftovi (encorafenib) or FOLFOX alone in colorectal cancer cell line xenograft models harboring BRAF V600E (PMID: 37040395). | 37040395 |
| BRAF V600E | melanoma | sensitive | AZD0364 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD0364 (ATG-017) inhibited cell growth, decreased phosphorylation of Erk target genes, and increased expression of apoptosis markers in melanoma cells harboring BRAF V600E in culture, and resulted in tumor regression in cell line xenograft models (PMID: 33273059). | 33273059 |
| BRAF V600E | colorectal cancer | sensitive | Chloroquine + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, combination treatment with Mekinist (trametinib) and Chloroquine resulted in tumor regression in a colorectal cancer patient-derived xenograft (PDX) model harboring BRAF V600E (PMID: 30833748). | 30833748 |
| BRAF V600E | uveal melanoma | no benefit | YM-254890 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed mouse melanocytes expressing BRAF V600E were insensitive to treatment with YM-254890 (PMID: 33229459). | 33229459 |
| BRAF V600E | skin melanoma | no benefit | YM-254890 | Preclinical - Cell culture | Actionable | In a preclinical study, YM-254890 treatment did not inhibit cell viability of a cutaneous melanoma cell line harboring BRAF V600E in culture (PMID: 33229459). | 33229459 |
| BRAF V600E | skin melanoma | no benefit | Trametinib + YM-254890 | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with YM-254890 and Mekinist (trametinib) did not result in synergistic inhibition of cell viability of a cutaneous melanoma cell line harboring BRAF V600E in culture (PMID: 33229459). | 33229459 |
| BRAF V600E | melanoma | sensitive | Lifirafenib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination treatment of Mekinist (trametinib) and Lifirafenib (BGB-283) led to greater inhibition of growth in melanoma cell lines harboring BRAF V600E in culture compared to either treatment alone (PMID: 33318037). | 33318037 |
| BRAF V600E | colorectal cancer | sensitive | Lifirafenib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination treatment of Mekinist (trametinib) and Lifirafenib (BGB-283) led to greater inhibition of growth in a colorectal cancer cell line harboring BRAF V600E in culture compared to either treatment alone (PMID: 33318037). | 33318037 |
| BRAF V600E | melanoma | predicted - sensitive | PF-07284890 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PF-07284890 treatment led to inhibition of tumor growth, tumor regression, and survival benefit in an intracranial model, and tumor growth inhibition in a subcutaneous cell line xenograft model of melanoma harboring BRAF V600E (Cancer Res 2021;81(13_Suppl):Abstract nr 1473). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | Cetuximab + Encorafenib + PF-07284892 | Case Reports/Case Series | Actionable | In a clinical case study, the combination of PF-07284892, Erbitux (cetuximab), and Braftovi (encorafenib) resulted in a 30% tumor reduction in a colorectal cancer patient harboring BRAF V600E, who remained on treatment for 6 months, and the combination inhibited tumor growth in a cell line xenograft model (PMID: 37269335; NCT04800822). | 37269335 |
| BRAF V600E | colon adenocarcinoma | predicted - sensitive | Dabrafenib + Regorafenib + Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in a patient with colon adenocarcinoma harboring BRAF V600E led to stable disease, and treatment continued for eight months, at which time some disease progression was observed (PMID: 33568355). | 33568355 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + Regorafenib + Trametinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in a melanoma cell line harboring BRAF V600E resulted in suppression of colony formation in culture, and suppressed tumor growth in patient-derived xenograft (PDX) models (PMID: 33568355). | 33568355 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + Regorafenib + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Stivarga (regorafenib), Tafinlar (dabrafenib), and Mekinist (trametinib) in colorectal cancer cell lines harboring BRAF V600E resulted in suppression of colony formation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 33568355). | 33568355 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + LXH 254 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with LXH 254, Tafinlar (dabrafenib), and Mekinist (trametinib) in a melanoma cell line harboring BRAF V600E resulted in suppression of colony formation in culture (PMID: 33568355). | 33568355 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + LXH 254 + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with LXH 254, Tafinlar (dabrafenib), and Mekinist (trametinib) in colorectal cancer cell lines harboring BRAF V600E resulted in suppression of colony formation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 33568355). | 33568355 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + RAF709 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with RAF709, Tafinlar (dabrafenib), and Mekinist (trametinib) in melanoma cell line harboring BRAF V600E resulted in suppression of colony formation in culture (PMID: 33568355). | 33568355 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + RAF709 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with RAF709, Tafinlar (dabrafenib), and Mekinist (trametinib) in colorectal cancer cell lines harboring BRAF V600E resulted in suppression of colony formation in culture (PMID: 33568355). | 33568355 |
| BRAF V600E | melanoma | no benefit | RM-018 | Preclinical - Cell culture | Actionable | In a preclinical study, RM-018 did not inhibit growth of melanoma cells harboring BRAF V600E in culture (PMID: 33824136). | 33824136 |
| BRAF V600E | hairy cell leukemia | predicted - sensitive | Ruxolitinib + Vemurafenib | Phase II | Actionable | In a Phase II trial (HCL-PG03), combined Zelboraf (vemurafenib) and Jakafi (ruxolitinib) therapy in relapsed or refractory hairy cell leukemia patients with BRAF V600E demonstrated safety, and led to complete response (CR) in 87% (26/30) of patients, including 17 (65%) with negative minimal residual disease, a progression-free survival rate of 78% at a median follow-up of 37 months, and a relapse-free survival rate of 85% in the 26 patients with a CR at a median follow-up of 34 months (PMID: 33979489). | 33979489 |
| BRAF V600E | endometrial adenocarcinoma | predicted - sensitive | Dabrafenib + Rabeprazole + Rifampin + Trametinib | Case Reports/Case Series | Actionable | In a Phase I trial, the addition of Mekinist (trametinib) to combination treatment with Tafinlar (dabrafenib), Rabeprazole, and Rifampin resulted in a maintained radiographic response of lung metastases and stable pelvic mass size in a patient with metastatic endometrial adenocarcinoma harboring BRAF V600E, which lasted for 12 months (PMID: 33537843; NCT01954043). | 33537843 |
| BRAF V600E | melanoma | sensitive | KRT-232 + Navitoclax | Preclinical - Pdx | Actionable | In a preclinical study, the combination of KRT-232 (AMG 232) and Navitoclax (ABT-263) resulted in a greater response than either drug alone in patient-derived xenograft (PDX) models of melanoma harboring BRAF V600E, leading to tumor regression (PMID: 32234759). | 32234759 |
| BRAF V600E | melanoma | sensitive | ASTX029 + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with ASTX029 and Zelboraf (vemurafenib) resulted in decreased viability of melanoma cells harboring BRAF V600E compared to either agent alone in culture (PMID: 34330842). | 34330842 |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Cobimetinib + Gemcitabine + Nab-paclitaxel | Case Reports/Case Series | Actionable | In a clinical case study, Gemzar (gemcitabine), Abraxane (nab-paclitaxel), and Cotellic (cobimetinib) combination treatment resulted in a complete radiologic response within 6 months of initiation lasting at least 16 months in a patient with microsatellite stable, KRAS wild-type pancreatic ductal adenocarcinoma harboring BRAF V600E (PMID: 34667063). | 34667063 |
| BRAF V600E | high grade glioma | sensitive | LY3009120 + Vemurafenib | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Zelboraf (vemurafenib) and LY3009120 treatment led to greater inhibition of cell growth compared to either agent alone in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| BRAF V600E | high grade glioma | predicted - sensitive | Vemurafenib + ZM336372 | Preclinical - Patient cell culture | Actionable | In a preclinical study, combination treatment with Zelboraf (vemurafenib) and ZM336372 treatment led to inhibition of cell growth in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| BRAF V600E | colorectal cancer | predicted - sensitive | Cetuximab + Encorafenib + ERAS-007 | Case Reports/Case Series | Actionable | In a Phase Ib/II trial (HERKULES), combination treatment with ERAS-007, Erbitux (cetuximab), and Braftovi (encorafenib) demonstrated safety and activity in patients with metastatic colorectal cancer harboring BRAF V600E, resulting in 1 confirmed and 1 unconfirmed partial response of 4 efficacy evaluable patients (J Clin Oncol 41, 2023 (suppl 16; abstr 3557); NCT05039177). | detail... |
| BRAF V600E | triple-receptor negative breast cancer | predicted - sensitive | Nab-paclitaxel + Vemurafenib | Case Reports/Case Series | Actionable | In a clinical case study, Zelboraf (vemurafenib) and Abraxane (nab-paclitaxel) combination treatment resulted in regression of some metastatic pulmonary lesions and a progression-free survival of 4.4 months in a patient with triple-negative breast cancer harboring BRAF V600E, but a biopsy in lesions that progressed showed acquisition of additional mutations in PDGFRB, NF2, GRM3, MLH1, FOXA1, LRP1B, and AR amplification (PMID: 34818649). | 34818649 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Trametinib + Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ulixertinib (BVD-523) and Mekinist (trametinib) had a synergistic effect on the induction of apoptosis in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture (PMID: 35882450). | 35882450 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, PF-07799933 treatment resulted in a complete response in a patient with pleomorphic xanthoastrocytoma harboring BRAF V600E (PMID: 38691346; NCT05355701). | 38691346 |
| BRAF V600E | colorectal cancer | predicted - sensitive | PF-07799933 | Preclinical - Biochemical | Actionable | In a preclinical study, PF-07799933 inhibited Erk phosphorylation in colorectal cancer cells harboring BRAF V600E in culture (PMID: 38691346). | 38691346 |
| BRAF V600E | melanoma | predicted - sensitive | Binimetinib + PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with the combination of PF-07799933 and Mektovi (binimetinib) resulted in a partial response in 2 patients with melanoma harboring BRAF V600E and stable disease in 1 patient (PMID: 38691346; NCT05355701). | 38691346 |
| BRAF V600E | high grade glioma | predicted - sensitive | Binimetinib + PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, the addition of Mektovi (binimetinib) to treatment with PF-07799933 resulted in a partial response in a patient with high grade glioma harboring BRAF V600E (PMID: 38691346; NCT05355701). | 38691346 |
| BRAF V600E | colon cancer | predicted - sensitive | ABM-1310 + Cetuximab | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with ABM-1310 and Erbitux (cetuximab) led to inhibition of tumor growth in a colon cancer cell line xenograft model harboring BRAF V600E (Cancer Res (2020) 80 (16_Supplement): 4038). | detail... |
| BRAF V600E | colon cancer | predicted - sensitive | ABM-1310 + Binimetinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with ABM-1310 and Mektovi (binimetinib) led to inhibition of tumor growth in a colon cancer cell line xenograft model harboring BRAF V600E (Cancer Res (2020) 80 (16_Supplement): 4038). | detail... |
| BRAF V600E | melanoma | predicted - sensitive | IMM-1-104 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IMM-1-104 treatment led to tumor growth inhibition in a cell line xenograft model of melanoma harboring BRAF V600E (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P252). | detail... |
| BRAF V600E | melanoma | predicted - sensitive | CFT1946 | Phase I | Actionable | In a Phase I trial, CFT1946 treatment demonstrated safety and preliminary activity in patients with advanced solid tumors (n=25) including melanoma (40%), colorectal cancer (40%), non-small cell lung cancer (8%), and other non-CNS tumors harboring BRAF V600E (n=22), V600K (n=2), or V600R (n=1), with 1 unconfirmed partial response (uPR) and 7 stable diseases in efficacy evaluable patients (n=14) at data cutoff, and 1 additional uPR after data cutoff (Ann Oncol (2024) 35 (Suppl_2): S490-S491; NCT05668585). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | Cetuximab + Encorafenib + Ulixertinib | Case Reports/Case Series | Actionable | In an expanded access program (ULI-EAP-100), Ulixertinib (BVD-523), Braftovi (encorafenib), and Erbitux (cetuximab) combination therapy resulted in a complete response in a patient with colorectal cancer harboring BRAF V600E (J Clin Oncol 40, no. 16_suppl (June 01, 2022) e15101; NCT04566393). | detail... |
| BRAF V600E | low grade glioma | predicted - sensitive | FCN-159 | Phase II | Actionable | In a Phase II trial, FCN-159 treatment was well tolerated and resulted in 6 partial responses, 9 minor responses, and 7 with stable disease in 22 pediatric patients with low-grade glioma harboring BRAF V600E (12/23), KIAA1549-BRAF (8/23), or NF1 mutations (3/23) (Ann Oncol (2023) 34 (suppl_2): S391-S392). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Pyrvinium + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Zelboraf (vemurafenib) and Pyrvinium resulted in decreased viability in colorectal cancer cell lines harboring BRAF V600E in culture, and led to synergistic inhibition of tumor growth in a cell line xenograft model (PMID: 36198029). | 36198029 |
| BRAF V600E | colorectal cancer | sensitive | Axitinib + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination treatment with Zelboraf (vemurafenib) and Inlyta (axitinib) resulted in decreased cell viability in colorectal cancer cell lines harboring BRAF V600E in culture, and led to synergistic inhibition of tumor growth in cell line xenograft models (PMID: 36198029). | 36198029 |
| BRAF V600E | colorectal cancer | sensitive | Panobinostat + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Farydak (panobinostat) synergistically inhibited cell viability and induced apoptosis in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Trametinib + Vorinostat | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Zolinza (vorinostat) resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Romidepsin + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Istodax (romidepsin) resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Mocetinostat + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Mocetinostat (MGCD0103) resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Entinostat + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Entinostat (MS-275) resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Trametinib + Valproic acid | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Mekinist (trametinib) and Valproic acid resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | colorectal cancer | sensitive | Panobinostat + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Farydak (panobinostat) resulted in greater apoptotic activity compared to either agent alone in a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 36343387). | 36343387 |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Binimetinib + Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Ulixertinib (BVD-523) and Mektovi (binimetinib) inhibited proliferation and had a synergistic effect on induction of apoptosis and inhibition of MAPK pathway activity in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture, and improved the progressive disease/partial response ratio compared to either drug alone in a zebrafish xenograft model (PMID: 35882450). | 35882450 |
| BRAF V600E | pleomorphic xanthoastrocytoma | predicted - sensitive | Selumetinib + Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ulixertinib (BVD-523) and Koselugo (selumetinib) inhibited proliferation in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture (PMID: 35882450). | 35882450 |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Ulixertinib + Vinblastine | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Ulixertinib (BVD-523) and Velban (vinblastine) inhibited proliferation and had a synergistic effect on induction of apoptosis in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture (PMID: 35882450). | 35882450 |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Navitoclax + Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Ulixertinib (BVD-523) and Navitoclax (ABT-263) synergistically induced apoptosis in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture, and improved the partial response rate compared to either drug alone in a zebrafish xenograft model (PMID: 35882450). | 35882450 |
| BRAF V600E | melanoma | predicted - sensitive | DS03090629 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, DS03090629 inhibited Erk and Mek phosphorylation and proliferation in a melanoma cell line harboring BRAF V600E in culture and led to tumor stasis in a cell line xenograft model (PMID: 36622773). | 36622773 |
| BRAF V600E | melanoma | sensitive | Dabrafenib + DS03090629 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of DS03090629 and Tafinlar (dabrafenib) inhibited Erk phosphorylation and proliferation in a melanoma cell line harboring BRAF V600E in culture and induced tumor regression in a cell line xenograft model (PMID: 36622773). | 36622773 |
| BRAF V600E | colorectal cancer | sensitive | Saracatinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Saracatinib (AZD0530) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Dasatinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Sprycel (dasatinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Bosutinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Bosulif (bosutinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Dasatinib + Gefitinib + Vemurafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib), Iressa (gefitinib), and Sprycel (dasatinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture and resulted in greater tumor growth inhibition and tumor regression in patient-derived xenograft (PDX) models to a greater degree than the doublet combinations of Zelboraf (vemurafenib) and Iressa (gefitinib) or Zelboraf (vemurafenib) and Sprycel (dasatinib) (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Zelboraf (vemurafenib) and Celecoxib synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Gefitinib + Trametinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Celecoxib to the combination of Zelboraf (vemurafenib), Mekinist (trametinib), and Iressa (gefitinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Trametinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Celecoxib to the combination of Zelboraf (vemurafenib) and Mekinist (trametinib) synergistically inhibited viability in colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Dabrafenib + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, the addition of Celecoxib to the combination of Tafinlar (dabrafenib) and Mekinist (trametinib) inhibited tumor growth and induced tumor regression in colorectal cancer patient-derived xenograft (PDX) models harboring BRAF V600E (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Dabrafenib + Panitumumab + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, the addition of Celecoxib to the combination of Tafinlar (dabrafenib), Mekinist (trametinib), and Vectibix (panitumumab) inhibited tumor growth and induced tumor regression in colorectal cancer patient-derived xenograft (PDX) models harboring BRAF V600E (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Celecoxib + Encorafenib + Panitumumab | Preclinical - Pdx | Actionable | In a preclinical study, the addition of Celecoxib to the combination of Braftovi (encorafenib) and Vectibix (panitumumab) inhibited tumor growth and induced tumor regression in colorectal cancer patient-derived xenograft (PDX) models harboring BRAF V600E to a greater degree than the combination of Braftovi (encorafenib) and Vectibix (panitumumab) (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Dasatinib + Gefitinib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720, Iressa (gefitinib), and Sprycel (dasatinib) inhibited tumor growth in colorectal cancer cell line xenograft models harboring BRAF V600E to a greater degree than the combinations of PLX4720 and Iressa (gefitinib) or PLX4720 and Sprycel (dasatinib) (PMID: 36759733). | 36759733 |
| BRAF V600E | colorectal cancer | sensitive | Gefitinib + PLX4720 + Saracatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PLX4720, Iressa (gefitinib), and Saracatinib (AZD0530) inhibited tumor growth in colorectal cancer cell line xenograft models harboring BRAF V600E to a greater degree than the combinations of PLX4720 and Iressa (gefitinib) or PLX4720 and Saracatinib (AZD0530) (PMID: 36759733). | 36759733 |
| BRAF V600E | melanoma | predicted - sensitive | PHI-501 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PHI-501 inhibited growth and migration and induced apoptosis in a melanoma cell line harboring BRAF V600E and induced dose-dependent tumor growth inhibition in a cell line xenograft model (Cancer Res (2023) 83 (7_Supplement): 1627). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Encorafenib + PF-07284892 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PF-07284892, Mektovi (binimetinib), and Braftovi (encorafenib) inhibited Erk phosphorylation in colorectal cancer cells harboring BRAF V600E in culture and induced tumor regression in a cell line xenograft model (PMID: 37269335). | 37269335 |
| BRAF V600E | colon cancer | sensitive | IHMT-RAF-128 | Preclinical - Cell culture | Actionable | In a preclinical study, IHMT-RAF-128 inhibited proliferation in a colon cancer cell line harboring BRAF V600E in culture (PMID: 37164118). | 37164118 |
| BRAF V600E | melanoma | sensitive | IHMT-RAF-128 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IHMT-RAF-128 inhibited proliferation and induced cell cycle arrest and apoptosis in melanoma cell lines harboring BRAF V600E in culture and inhibited tumor growth in a cell line xenograft model (PMID: 37164118). | 37164118 |
| BRAF V600E | Advanced Solid Tumor | sensitive | IHMT-RAF-128 | Preclinical - Cell culture | Actionable | In a preclinical study, IHMT-RAF-128 inhibited proliferation of a cell line expressing BRAF V600E in culture (PMID: 37164118). | 37164118 |
| BRAF V600E | colorectal cancer | sensitive | Binimetinib + Trifluridine-tipiracil hydrochloride | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Mektovi (binimetinib) enhanced the efficacy of Lonsurf (trifluridine/tipiracil hydrochloride) treatment and synergistically inhibited proliferation in colorectal cancer cells harboring BRAF V600E in culture (PMID: 28551618). | 28551618 |
| BRAF V600E | colorectal cancer | no benefit | Cetuximab + Fluorouracil + Leucovorin + Vemurafenib | Phase II | Actionable | In a Phase II trial (MODUL), patients with metastatic colorectal cancer harboring BRAF V600E did not demonstrate improved progression-free survival when treated with the combination of Zelboraf (vemurafenib), Erbitux (cetuximab), Adrucil (fluorouracil), and Wellcovorin (leucovorin) compared to the control treatment of Avastin (bevacizumab) with a fluoropyrimidine (HR=0.95 and P=0.872) (PMID: 36921494; NCT02291289). | 36921494 |
| BRAF V600E | colorectal cancer | sensitive | SJ-C1044 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, SJ-C1044 decreased growth in a colorectal cancer cell line harboring BRAF V600E in culture and inhibited tumor growth in a cell line xenograft model (PMID: 37504287). | 37504287 |
| BRAF V600E | melanoma | sensitive | Tunlametinib + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of Tunlametinib (HL-085) and Zelboraf (vemurafenib) synergistically inhibited proliferation of a melanoma cell line harboring BRAF V600E in culture, and synergistically inhibited tumor growth in a cell line xenograft model (PMID: 37808191). | 37808191 |
| BRAF V600E | colorectal cancer | sensitive | Tunlametinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of Tunlametinib (HL-085) and Zelboraf (vemurafenib) synergistically inhibited proliferation of a colorectal cancer cell line harboring BRAF V600E in culture (PMID: 37808191). | 37808191 |
| BRAF V600E | melanoma | sensitive | SIJ777 | Preclinical - Cell culture | Actionable | In a preclinical study, SIJ777 inhibited Mek, Erk, and Akt phosphorylation, proliferation, migration, and invasion, and induced apoptosis in melanoma cell lines harboring BRAF V600E in culture (PMID: 33917428). | 33917428 |
| BRAF V600E | melanoma | sensitive | Encorafenib + Talazoparib | Preclinical - Patient cell culture | Actionable | In a preclinical study, treatment with the combination of Talzenna (talazoparib) and Braftovi (encorafenib) synergistically inhibited viability of patient-derived melanoma spheroids harboring BRAF V600E in culture (PMID: 37729428). | 37729428 |
| BRAF V600E | melanoma | sensitive | Binimetinib + Encorafenib + Talazoparib | Preclinical - Patient cell culture | Actionable | In a preclinical study, treatment with the combination of Talzenna (talazoparib), Braftovi (encorafenib), and Mektovi (binimetinib) synergistically inhibited viability of patient-derived melanoma spheroids harboring BRAF V600E in culture (PMID: 37729428). | 37729428 |
| BRAF V600E | melanoma | sensitive | AZD3514 + Dabrafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of AZD3514 to Tafinlar (dabrafenib) treatment inhibited colony formation in melanoma cell lines harboring BRAF V600E in culture (PMID: 37838724). | 37838724 |
| BRAF V600E | melanoma | sensitive | ARCC4 + Dabrafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of ARCC4 to Tafinlar (dabrafenib) treatment inhibited colony formation in melanoma cell lines harboring BRAF V600E in culture (PMID: 37838724). | 37838724 |
| BRAF V600E | melanoma | predicted - sensitive | IMM-6-415 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IMM-6-415 treatment inhibited tumor growth in a cell line xenograft model of melanoma harboring BRAF V600E (Mol Cancer Ther (2023) 22 (12_Supplement): A093). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | IMM-6-415 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IMM-6-415 treatment inhibited tumor growth in a cell line xenograft model of colorectal cancer harboring BRAF V600E (Mol Cancer Ther (2023) 22 (12_Supplement): A093). | detail... |
| BRAF V600E | melanoma | predicted - sensitive | Encorafenib + IMM-6-415 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of Braftovi (encorafenib) and IMM-6-415 resulted in increased tumor growth inhibition compared to the combination of Mektovi (binimetinib) and Braftovi (encorafenib) in a cell line xenograft model of melanoma harboring BRAF V600E (Mol Cancer Ther (2023) 22 (12_Supplement): A093). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | Encorafenib + IMM-6-415 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of Braftovi (encorafenib) and IMM-6-415 resulted in increased tumor growth inhibition compared to the combination of Mektovi (binimetinib) and Braftovi (encorafenib) in a cell line xenograft model of colorectal cancer harboring BRAF V600E (Mol Cancer Ther (2023) 22 (12_Supplement): A093). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + IAG933 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of IAG933 and Tafinlar (dabrafenib) inhibited proliferation of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 38565920). | 38565920 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + IAG933 + LTT462 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of IAG933, Tafinlar (dabrafenib), and LTT462 inhibited proliferation of colorectal cancer cell lines harboring BRAF V600E in culture and resulted in greater tumor growth inhibition compared to either agent alone in a cell line xenograft model (PMID: 38565920). | 38565920 |
| BRAF V600E | colorectal cancer | sensitive | Dabrafenib + IAG933 + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of IAG933, Tafinlar (dabrafenib), and Mekinist (trametinib) inhibited proliferation of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 38565920). | 38565920 |
| BRAF V600E | melanoma | sensitive | Ravoxertinib + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of Ravoxertinib (GDC-0994) and Zelboraf (vemurafenib) resulted in additive effects, with decreased growth of a melanoma cell line harboring BRAF V600E in culture (PMID: 38728872). | 38728872 |
| BRAF V600E | melanoma | predicted - sensitive | Binimetinib + PLX8394 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of Mektovi (binimetinib) and PLX8394 inhibited viability of melanoma cells harboring BRAF V600E in culture (Cancer Res (2024) 84 (6_Supplement): 4609). | detail... |
| BRAF V600E | colorectal cancer | predicted - sensitive | Binimetinib + PLX8394 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of Mektovi (binimetinib) and PLX8394 inhibited viability of colorectal cancer cells harboring BRAF V600E in culture (Cancer Res (2024) 84 (6_Supplement): 4609). | detail... |
| BRAF V600E | thyroid cancer | sensitive | PLX4720 + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of PLX4720 and Nexavar (sorafenib) inhibited proliferation of thyroid cancer cell lines harboring BRAF V600E in culture and resulted in greater tumor growth inhibition than PLX4720 alone in a cell line xenograft model (PMID: 38795180). | 38795180 |
| BRAF V600E | thyroid cancer | sensitive | Lenvatinib + PLX4720 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of PLX4720 and Lenvima (lenvatinib) inhibited proliferation of thyroid cancer cell lines harboring BRAF V600E in culture and resulted in greater tumor growth inhibition than PLX4720 alone in a cell line xenograft model (PMID: 38795180). | 38795180 |
| BRAF V600E | melanoma | sensitive | DSR6434 + unspecified PD-1 antibody + Vemurafenib | Preclinical | Actionable | In a preclinical study, treatment with the combination of Zelboraf (vemurafenib), DSR6434, and an anti-PD-1 antibody induced tumor regression and resulted in prolonged progression-free survival compared to either of the doublet combination therapies in a syngeneic mouse model of melanoma harboring BRAF V600E (PMID: 38894534). | 38894534 |
| BRAF V600E | melanoma | no benefit | RGT-018 | Preclinical - Cell culture | Actionable | In a preclinical study, RGT-018 did not inhibit proliferation of melanoma cells harboring BRAF V600E in 3D culture (PMID: 39087485). | 39087485 |
| BRAF V600E | colorectal cancer | sensitive | MTX-531 + Trametinib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Mekinist (trametinib) and MTX-531 inhibited tumor growth with a 40% partial response rate and increased survival in a patient-derived xenograft (PDX) model of colorectal cancer harboring BRAF V600E (PMID: 38992135). | 38992135 |
| BRAF V600E | glioblastoma | sensitive | PD-0325901 + Radiotherapy | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of PD-0325901 and radiotherapy synergistically inhibited cell growth of glioblastoma cell lines harboring BRAF V600E in culture (PMID: 38714355). | 38714355 |
| BRAF V600E | papillary thyroid carcinoma | sensitive | AZD1208 + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of Zelboraf (vemurafenib) and AZD1208 synergistically inhibited viability and colony formation of papillary thyroid carcinoma cell lines harboring BRAF V600E in culture (PMID: 38593698). | 38593698 |
| BRAF V600E | colorectal cancer | sensitive | Encorafenib + Tazemetostat | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Tazverik (tazemetostat) sensitized a colorectal cancer cell line harboring BRAF V600E to Braftovi (encorafenib) treatment in culture, resulting in decreased cell proliferation (PMID: 39121480). | 39121480 |
| BRAF V600E | colorectal cancer | sensitive | Cetuximab + Encorafenib + Tazemetostat | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Tazverik (tazemetostat) sensitized a colorectal cancer cell line harboring BRAF V600E to treatment with the combination of Braftovi (encorafenib) and Erbitux (cetuximab) in culture, resulting in decreased cell proliferation (PMID: 39121480). | 39121480 |