Therapy Detail
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| Therapy Name | Encorafenib |
| Synonyms | |
| Therapy Description |
Braftovi (encorafenib) is an inhibitor of Raf kinase with selective activity against BRAF V600E, resulting in growth inhibition (PMID: 24864047). Braftovi (encorafenib) is FDA approved for use in combination with Mektovi (binimetinib) in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, and in patients with metastatic non-small cell lung cancer harboring BRAF V600E, and in combination with Erbitux (cetuximab) in patients with metastatic colorectal cancer with BRAF V600E (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Encorafenib | Braftovi | LGX818 | BRAF Inhibitor 25 | Braftovi (encorafenib) is an inhibitor of Raf kinase with selective activity against BRAF V600E, resulting in growth inhibition (PMID: 24864047). Braftovi (encorafenib) is FDA approved for use in combination with Mektovi (binimetinib) in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, and in patients with metastatic non-small cell lung cancer harboring BRAF V600E, and in combination with Erbitux (cetuximab) in patients with metastatic colorectal cancer with BRAF V600E (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E MAP2K1 W247* | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 W247* in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 G79V | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G79V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R96K | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R96K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R49H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R49H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 M94I | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 M94I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S72G | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S72G in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 K57T | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 K57T was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Y134C | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Y134C in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 I103_K104del | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I103_K104del was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S86A | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S86A in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 I99_K104del | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I99_K104del was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R201C | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R201C in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P326H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P326H in culture (PMID: 36442478). | 36442478 |
| BRAF L485_P490delinsF | Advanced Solid Tumor | predicted - resistant | Encorafenib | Preclinical - Biochemical | Actionable | In a preclinical study, Braftovi (encorafenib) did not inhibit Mek and Erk phosphorylation in cells expressing BRAF L485_P490delinsF in culture (PMID: 37656784). | 37656784 |
| BRAF L597S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited ERK activation and proliferation of melanoma cell lines harboring BRAF L597S in culture (PMID: 29903896). | 29903896 |
| BRAF V600E MAP2K1 S200Y | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S200Y in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P306H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P306H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 G276W | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G276W in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 D351G | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D351G in culture (PMID: 36442478). | 36442478 |
| BRAF G469V | melanoma | no benefit | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) did not inhibit ERK phosphorylation or proliferation of a melanoma cell line harboring BRAF G469V (PMID: 29903896). | 29903896 |
| BRAF V600E MAP2K1 F53L | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53L was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S231L | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S231L in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P105_A106del | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P105_A106del was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V127M | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V127M in culture (PMID: 36442478). | 36442478 |
| BRAF L485_P490delinsY | Advanced Solid Tumor | predicted - resistant | Encorafenib | Preclinical - Biochemical | Actionable | In a preclinical study, Braftovi (encorafenib) did not inhibit Mek and Erk phosphorylation in cells expressing BRAF L485_P490delinsY in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 D136N | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D136N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S241Y | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S241Y in culture (PMID: 36442478). | 36442478 |
| BRAF mutant | melanoma | sensitive | Encorafenib | Phase I | Actionable | In a Phase I trial, Encorafenib (LGX818) treatment resulted in an overall response rate (ORR) of 60% (15/25) and a median progression-free survival (mPFS) of 12.4 months in BRAF inhibitor-naïve melanoma patients harboring BRAF mutations, and an ORR of 22% (6/29) and mPFS of 1.9 months in BRAF inhibitor-pretreated patients (PMID: 28611198; NCT01436656). | 28611198 |
| 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 | 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 L597V | lung adenocarcinoma | resistant | Encorafenib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were resistant to treatment with Braftovi (encorafenib) in culture (PMID: 32540409). | 32540409 |
| BRAF V600E MAP2K1 F53C | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53C was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A14S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A14S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P162S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P162S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Y229H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Y229H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R49C | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R49C in culture (PMID: 36442478). | 36442478 |
| BRAF L485_P490delinsFS | Advanced Solid Tumor | predicted - resistant | Encorafenib | Preclinical - Biochemical | Actionable | In a preclinical study, Braftovi (encorafenib) did not inhibit Mek and Erk phosphorylation in cells expressing BRAF L485_P490delinsFS in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 A76V | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A76V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 F53_Q58delinsL | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53_Q58delinsL was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 K57E | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 K57E was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P293S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P293S in culture (PMID: 36442478). | 36442478 |
| 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 MAP2K1 P193S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P193S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 N345T | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 N345T in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 E102_I103del | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E102_I103del was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V487_P492delinsA | pancreatic carcinoma | decreased response | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a pancreatic carcinoma cell line harboring BRAF V487_P492delinsA was less sensitive to Braftovi (encorafenib) treatment compared to type II RAF inhibitors in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 E367K | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E367K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 L63_D67del | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L63_D67del in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V154I | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V154I in culture (PMID: 36442478). | 36442478 |
| 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 MAP2K1 R349K | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R349K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V93F | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V93F in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 I310L | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I310L in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 D303N | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D303N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 E203K | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E203K was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 L215F | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L215F in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A106T | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A106T in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R291K | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R291K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 L115P | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L115P in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R108Q | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R108Q in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Q58* | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Q58* in culture (PMID: 36442478). | 36442478 |
| BRAF R239Q BRAF L597S | melanoma | sensitive | Encorafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited ERK activation and proliferation of patient-derived melanoma cells harboring BRAF L597S, as well as BRAF R239Q, in culture, and delayed tumor growth and induced shrinkage in 8% (1/12) of tumors in a melanoma patient-derived xenograft (PDX) model (PMID: 29903896). | 29903896 |
| BRAF V600E MAP2K1 G176S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G176S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 M146I | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 M146I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P264S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P264S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S327T | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S327T in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R47Q | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R47Q in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Q56_G61delinsR | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Q56_G61delinsR was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF N486_P490del | ovarian cancer | decreased response | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, an ovarian cancer cell line harboring BRAF N486_P490del was less sensitive to Braftovi (encorafenib) treatment compared to type II RAF inhibitors in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 L235H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L235H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 N382H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 N382H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 C121S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 C121S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S150F | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S150F in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V258I | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V258I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 H100_I103delinsPL | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 H100_I103delinsPL was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 G294E | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G294E in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 F53V | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53V was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S331R | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S331R in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S212N | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S212N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V60E | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V60E was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A132V | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A132V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P387S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P387S in culture (PMID: 36442478). | 36442478 |
| BRAF L485_P490delinsY | lung non-small cell carcinoma | decreased response | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a non-small cell lung cancer cell line harboring BRAF L485_P490delinsY was less sensitive to Braftovi (encorafenib) treatment compared to type II RAF inhibitors in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 K4N | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 K4N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 F53I | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53I was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 I103N | melanoma | resistant | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I103N was resistant to Braftovi (encorafenib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R201H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R201H in culture (PMID: 36442478). | 36442478 |
| BRAF S363F BRAF K601E | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited growth of a melanoma cell line harboring BRAF K601E, as well as BRAF S363F, in culture (PMID: 29903896). | 29903896 |
| BRAF V600E MAP2K1 D336H | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D336H in culture (PMID: 36442478). | 36442478 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT01777776 | Phase Ib/II | Encorafenib Encorafenib + Ribociclib | Safety and Efficacy of LEE011 and LGX818 in Patients With BRAF Mutant Melanoma. | Terminated | USA | NLD | CAN | AUS | 0 |
| NCT01894672 | Phase II | Encorafenib | BRAF Inhibitor, LGX818, Utilizing a Pulsatile Schedule in Patients With Stage IV or Unresectable Stage III Melanoma Characterized by a BRAFV600 Mutation | Completed | USA | 0 |
| NCT04801966 | Phase 0 | Palbociclib Alpelisib Atezolizumab Vemurafenib Ribociclib Talazoparib Cobimetinib Trametinib Abemaciclib Dabrafenib Nivolumab Binimetinib Pembrolizumab Encorafenib | Safety and Oversight of the Individually Tailored Treatment Approach: A Novel Pilot Study (TAILOR) | Terminated | AUS | 0 |
| NCT01436656 | Phase I | Encorafenib | A Phase I Study of Oral LGX818 in Adult Patients With Advanced or Metastatic BRAF Mutant Melanoma | Completed | USA | NOR | FRA | ESP | CHE | AUS | 1 |
| NCT01909453 | Phase III | Vemurafenib Encorafenib Binimetinib + Encorafenib | Study Comparing Combination of LGX818 Plus MEK162 Versus Vemurafenib and LGX818 Monotherapy in BRAF Mutant Melanoma (COLUMBUS) | Completed | USA | TUR | SWE | SVK | POL | NOR | NLD | ITA | ISR | HUN | GRC | GBR | FRA | ESP | DEU | CZE | CHE | CAN | BRA | AUS | ARG | 8 |
| NCT01981187 | Phase II | Encorafenib | LGX818 for Patients With BRAFV600 Mutated Tumors | Terminated | USA | 0 |
| NCT05203172 | FDA approved | Encorafenib Binimetinib + Encorafenib Binimetinib + Encorafenib + Ribociclib Binimetinib + Cetuximab + Encorafenib Binimetinib | The FLOTILLA Study: Providing Continued Access to The Study Medicines Encorafenib and Binimetinib for Participants in Prior Clinical Trials | Recruiting | USA | SVK | NLD | ITA | ISR | HUN | GBR | FRA | ESP | DEU | CZE | CAN | BRA | AUS | 4 |
| NCT05725200 | Phase II | Dasatinib Palbociclib Gemcitabine Trastuzumab Cetuximab Pertuzumab Panobinostat Alectinib Venetoclax Larotrectinib Encorafenib Everolimus Idelalisib Crizotinib Pembrolizumab Methotrexate Talazoparib | Study to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer (EVIDENT) | Recruiting | NOR | 0 |
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