molecules of the month


sel. CCR2 chemokine receptor antagonist

oral efficacy (25 mpk BID) in inflamm. models

from PK opt. of prior candidate

ACS Med. Chem. Lett., May 25, 2021

Bristol Myers Squibb, Princeton, NJ

1 min read

The BMS CCR2 inhibitor, BMS-753426, is a potent, oral follow-up molecule to prior clinical candidate, BMS-741672. A small change from a methyl and isopropyl-substituted tertiary amine to a t-butyl secondary amine led to a significant improvement in PK properties including lower clearance and higher bioavailability across species, including cyno. The compound has four nitrogen-bearing stereocenters but >100 g were prepared without a single column chromatography purification. The authors suggest that dual CCR2 and CCR5 inhibition may be more successful in various indications, and the related molecule BMS-813160 is a dual antagonist in several clinical trials.

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