molecules of the month


oral FGFR inhibitor

Ph. I candidate for solid tumors

opt. from previously disclosed lead

Bioorg. Med. Chem.

Astellas Pharma Inc.

oral FGFR inhibitor - Astellas Pharma Inc.
2 mins read

Context. ASP5878 (Astellas Pharma Inc.) is an oral pan-FGFR inhibitor. The four FGFRs have emerged as attractive targets for cancer in recent years, and we’ve covered several recently. FGFR3 has had less dedicated effort disclosed on it specifically relative to FGFRs 1, 2, and 4, but genetic alterations of FGFR3 have been noted in bladder cancer. In late-stage metastatic bladder cancer, metastasis to the brain is an issue that is not addressed well with antibodies or ADCs. This program targeted a brain-penetrant FGFR3 inhibitor (regardless of FGFR selectivity) while addressing hERG cardiotoxicity concerns of a previous pan-FGFR lead. ASP5878 entered a phase I clinical trial for the treatment of urothelial carcinoma, hepatocellular carcinoma and squamous cell lung carcinoma patients in…

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