enbezotinib

Enbezotinib is an orally bioavailable, macrocyclic small‑molecule tyrosine kinase inhibitor that selectively targets rearranged during transfection (RET) fusions and activating mutations, while also inhibiting SRC family kinases, for the treatment of RET‑altered cancers.[1][2][13][16] By binding RET in its active conformation, it potently inhibits RET autophosphorylation and downstream signaling, including in solvent‑front and other resistance mutations that limit first‑generation RET inhibitors, and SRC inhibition may further suppress bypass signaling pathways implicated in acquired resistance.[1][2][11][13][15][16] Enbezotinib was originally developed by Turning Point Therapeutics (acquired by Bristol Myers Squibb) and entered phase 1/2 clinical evaluation (NCT04161391) in advanced solid tumors with RET alterations (e.g., non‑small cell lung cancer and thyroid cancers), but this trial was terminated after an unfavorable risk–benefit assessment and the program has been discontinued.[2][4][12][13][16]

Other names

Enbezotinib