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Agerafenib is an orally bioavailable, selective multikinase inhibitor that targets mutant forms, fusions, and rearrangements involving the proto-oncogene receptor tyrosine kinase RET (rearranged during transfection), as well as the serine/threonine-protein kinase BRAF and epidermal growth factor receptor (EGFR). It is a small molecule developed for its potential antineoplastic activity in solid tumors. Agerafenib specifically inhibits mutated BRAF (notably V600E), RET, and EGFR kinases, thereby blocking downstream signaling through the RAF/MEK/ERK pathway. This inhibition leads to decreased proliferation of tumor cells harboring these mutations or alterations. The drug has been investigated primarily for cancers with RET alterations and other solid tumors such as malignant melanoma and colorectal cancer[1][2][3][4][5][7].
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