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Therapy Name | Binimetinib + Exarafenib |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Binimetinib | Mektovi | ARRY-162|ARRY-438162|MEK162 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mektovi (binimetinib) inhibits MEK1 and MEK2 resulting in inhibition of growth factor-mediated signaling and decreased tumor cell proliferation (PMID: 23587417). Mektovi (binimetinib) in combination with Braftovi (encorafenib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov). |
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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
NRAS act mut | melanoma | predicted - sensitive | Binimetinib + Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with the combination of Exarafenib (KIN-2787) and Mektovi (binimetinib) demonstrated safety in patients with NRAS-mutant melanoma (n=39) or other advanced solid tumors driven by BRAF class I or II alterations (n=10 and n=3) and resulted in a partial response in 35.5% (11/31, 9 confirmed partial responses) of efficacy evaluable NRAS-mutant melanoma patients (Ann Oncol (2024) 35 (Suppl_2): S491-S492; NCT04913285). | detail... |
NRAS act mut | melanoma | predicted - sensitive | Binimetinib + Exarafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Exarafenib (KIN-2787) and Mektovi (binimetinib) combination treatment inhibited growth of melanoma cell lines harboring NRAS mutations in culture, and resulted in improved tumor growth inhibition and Mapk pathway suppression in cell line xenograft models compared to either agent alone (J Clin Oncol 40, 2022 (suppl 16; abstr e15099)). | detail... |
BRAF fusion | Advanced Solid Tumor | predicted - sensitive | Binimetinib + Exarafenib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with the combination of Exarafenib (KIN-2787) and Mektovi (binimetinib) demonstrated safety in patients with NRAS-mutant melanoma (n=39) or other advanced solid tumors driven by BRAF class I or II alterations (n=10 and n=3) and resulted in one confirmed and one unconfirmed partial response in patients harboring BRAF fusions (n=3) (Ann Oncol (2024) 35 (Suppl_2): S491-S492; NCT04913285). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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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 |