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molecules of the year

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

FGF401-(roblitinib)
1 min read

September’s molecule, the Novartis FGFR4 inhibitor FGF401 (roblitinib), is a highly selective, reversible-covalent kinase inhibitor. The FGFR4 receptor has been a hot target recently due to its role in driving 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 irreversible covalent starting points and pursued a potentially safer reversible-covalent strategy instead. The aldehyde of roblitinib targets a unique Cys by the hinge region of the protein (GK+2) that is not present in the other FGFR’s and is present in only 4 other kinases. It is impressive that they were able to optimize an aldehyde for clinical oral…


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