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Tasurgratinib is an orally available, selective small molecule tyrosine kinase inhibitor that targets fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. It was discovered by Eisai’s Tsukuba Research Laboratories. Tasurgratinib inhibits the FGF/FGFR pathway by selectively interfering with the binding of FGF to its receptor, leading to inhibition of downstream signaling involved in tumor cell proliferation and survival. This mechanism results in antitumor activity, particularly in cancers harboring FGFR genetic aberrations such as gene fusions or rearrangements. The drug has demonstrated efficacy in patients with unresectable biliary tract cancer (including cholangiocarcinoma) with FGFR2 gene fusions or rearrangements who have progressed after chemotherapy. Tasurgratinib is marketed under the brand name TASFYGO for this indication in Japan and is also being investigated for other solid tumors and HER2-negative breast cancer[1][2][3][5][6][7].
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