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Fanregratinib (HMPL-453) is a novel, highly selective and potent small molecule inhibitor targeting fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. It acts by binding to and inhibiting these receptors, thereby blocking aberrant FGFR signaling pathways that drive tumor growth, angiogenesis promotion, and resistance to anti-tumor therapies. Fanregratinib is being developed primarily for the treatment of advanced intrahepatic cholangiocarcinoma (IHCC) patients with FGFR2 fusion or rearrangement. The drug has demonstrated superior potency and kinase selectivity compared to other drugs in its class in preclinical studies. Clinical development includes Phase II registration trials in IHCC as well as studies in other solid tumors such as malignant mesothelioma. HUTCHMED retains all worldwide rights to fanregratinib.
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