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Therapy Name Binimetinib + Exarafenib
Synonyms
Therapy Description

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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).

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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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...

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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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