molecules of the month


potent, selective, oral FPR2 GPCR agonist

for heart failure prevent. / entered Ph. I in HV

from optimization of known ligand

J. Med. Chem., May 24, 2020

Kyorin Pharmaceutical / Bristol-Myers Squibb

1 min read

BMS-986235/LAR-1219 is an FPR1-sparing FPR2-selective agonist intended to help resolve chronic inflammation/promote wound healing to prevent serious complications like heart failure. It’s a very efficient molecule and is orally efficacious in a mouse myocardial infarction model at doses as low as 0.3 mg/pk, despite having 3 N-H donors (urea + amide) in its core. Like DS-1971a it has a PK disconnect between species (significantly lower clearance in higher species than in rodents) but was successfully taken into development. Human data hasn’t been reported yet.

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