Therapy Detail
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| Therapy Name | Exarafenib |
| Synonyms | |
| Therapy Description |
Exarafenib (KIN-2787) is a small molecule pan-RAF inhibitor with activity against BRAF Class II and Class III mutants, which inhibits downstream signaling, potentially resulting in decreased growth of BRAF-mutant tumors (J Clin Oncol 39, no. 15_suppl (May 20, 2021) 3116-3116). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Exarafenib | KIN-2787|KIN2787|KIN 2787 | RAF Inhibitor (Pan) 28 | Exarafenib (KIN-2787) is a small molecule pan-RAF inhibitor with activity against BRAF Class II and Class III mutants, which inhibits downstream signaling, potentially resulting in decreased growth of BRAF-mutant tumors (J Clin Oncol 39, no. 15_suppl (May 20, 2021) 3116-3116). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF class 2 | Advanced Solid Tumor | predicted - sensitive | Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Exarafenib (KIN-2787) was tolerated and resulted in a partial response in 17.6% (6/34) and stable disease in 23.5% (8/34) of patients with BRAF-driven advanced solid tumors or NRAS-driven melanoma, including a partial response in 1 patient harboring a BRAF class 2 mutation (Cancer Res (2023) 83 (8_Supplement): CT032; NCT04913285). | detail... |
| BRAF class 3 | Advanced Solid Tumor | predicted - sensitive | Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Exarafenib (KIN-2787) was tolerated and resulted in a partial response in 17.6% (6/34) and stable disease in 23.5% (8/34) of patients with BRAF-driven advanced solid tumors or NRAS-driven melanoma, including a partial response in 1 patient harboring a BRAF class 3 mutation (Cancer Res (2023) 83 (8_Supplement): CT032; NCT04913285). | detail... |
| BRAF class 2 | pancreatic cancer | predicted - sensitive | Exarafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Exarafenib (KIN-2787) treatment led to inhibition of tumor growth in a pancreatic cell line xenograft model harboring a BRAF class 2 mutation (J of Clin Oncol 39, no. 15_suppl (May 20, 2021) 3116-3116). | detail... |
| BRAF class 1 | Advanced Solid Tumor | predicted - sensitive | Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Exarafenib (KIN-2787) was tolerated and resulted in a partial response in 17.6% (6/34) and stable disease in 23.5% (8/34) of patients with BRAF-driven advanced solid tumors or NRAS-driven melanoma, including 3 partial responses in patients harboring BRAF class 1 mutations (Cancer Res (2023) 83 (8_Supplement): CT032; NCT04913285). | detail... |
| BRAF class 1 | melanoma | predicted - sensitive | Exarafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Exarafenib (KIN-2787) treatment led to inhibition of tumor growth in a melanoma cell line xenograft model harboring a BRAF class 1 mutation (J of Clin Oncol 39, no. 15_suppl (May 20, 2021) 3116-3116). | detail... |
| BRAF class 3 | melanoma | predicted - sensitive | Exarafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Exarafenib (KIN-2787) treatment led to inhibition of tumor growth in a melanoma cell line xenograft model harboring a BRAF class 3 mutation (J of Clin Oncol 39, no. 15_suppl (May 20, 2021) 3116-3116). | detail... |
| NRAS act mut | melanoma | predicted - sensitive | Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Exarafenib (KIN-2787) was tolerated and resulted in a partial response in 17.6% (6/34) and stable disease in 23.5% (8/34) of patients with BRAF-driven advanced solid tumors or NRAS-driven melanoma, including a partial response in 1 melanoma patient harboring an NRAS mutation (Cancer Res (2023) 83 (8_Supplement): CT032; NCT04913285). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04913285 | Phase I | Binimetinib + Exarafenib Exarafenib | A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors | Recruiting | USA | NLD | FRA | ESP | AUS | 3 |
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