FGF401 (roblitinib) is a highly selective, reversible-covalent inhibitor of the kinase FGFR4, a receptor that can drive progression of certain cancers. The Novartis team found that the FGFR4 protein has a high re-synthesis rate and therefore would require significant drug exposure to have a meaningful effect, so they deprioritized [...]
Roblitinib is an Orally Available Aldehyde Selective for FGFR4
FGF401 (roblitinib)
oral reversible-covalent FGFR4 kinase inhibitor first sel. FGFR4i in clinical studies; for HCC from biochemical HTS and SBDD J. Med. Chem., Oct. 1, 2020 Novartis, Basel, CH
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