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Brimarafenib is an orally available, selective small molecule inhibitor of both monomeric and dimeric forms of activating mutations in the serine/threonine-protein kinase BRAF (B-raf), including V600 and non-V600 BRAF mutations as well as RAF fusions. By binding to these mutant forms, brimarafenib inhibits BRAF-mediated signaling through the MAPK/ERK pathway, which is frequently dysregulated in human cancers and drives tumor cell proliferation and survival. Brimarafenib is being developed primarily for the treatment of solid tumors harboring relevant genetic alterations, such as melanoma, colorectal cancer, pancreatic cancer, non-small cell lung cancer, bile duct cancer (cholangiocarcinoma), and endometrial cancer. The drug is under clinical investigation by MapKure—a joint venture between SpringWorks Therapeutics and BeiGene—with development also involving BeiGene directly[1][2][3][4][7].
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