molecules of the month


oral LPA1 GPCR receptor antagonist

Ph. II candidate for IPF (60 mg BID)

from addressing tox. of prior candidate

Journal of Medicinal Chemistry

Bristol Myers Squibb, Princeton, NJ

Chemical structure of molecule BMS-986278
2 mins read

This month’s cover molecule, BMS-986278, is an LPA1 antagonist and oral (up to 125 mg BID) Ph. II clinical candidate for idiopathic pulmonary fibrosis (IPF) (NCT04308681). Reviewer and nominator Christian Kuttruff says: “While there are two approved molecules for the treatment of IPF (pirfenidone from Roche and nintedanib from BI), there is still a significant medical need for IPF/PF-ILD patients. Alongside current Phase III assets targeting IPF (Fibrogen’s pamrevlumab, Roche’s pentraxin and United Therapeutics’ teprostinil), this BMS LPAR1 antagonist is a promising compound in development for IPF due to the fact that their previous frontrunner molecule (BMS-986020) showed promising proof-of-efficacy in a 6 month Ph. II trial in IPF patients, slowing the decline of FVC by 69% vs. placebo. BMS-986020’s trial was stopped due…

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