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Zoligratinib (DEBIO-1347, CH5183284) is an orally available, highly selective small molecule inhibitor of fibroblast growth factor receptor subtypes 1, 2, and 3 (FGFR1–3). It acts as an ATP-competitive inhibitor that binds to the ATP-binding site of FGFR1–3 and blocks their kinase activity. This inhibition disrupts FGFR-mediated signal transduction pathways involved in tumor cell proliferation and angiogenesis. Zoligratinib demonstrates potent antitumor effects in preclinical models with FGFR genetic alterations—including mutations, amplifications, or fusions—and has shown clinical activity in patients with advanced solid tumors harboring such alterations. The drug is being developed primarily for unresectable or metastatic tumors with specific FGFR gene alterations[2][3][4][5][6][7]. Developed by Debiopharm.
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