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) 27 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 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 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 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...
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...
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...
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...

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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 | FRA | ESP | AUS 4


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