molecules of the month


oral PAR4 antagonist

Ph. II completed in thrombosis (discontinued)

HTS, potency, and PK opt.

J. Med. Chem.

Bristol-Myers Squibb, Princeton, NJ

BMS-986120 Chemical Structure oral PAR4 antagonist - Bristol-Myers Squibb, Princeton, NJ
5 mins read

Context. BMS-986120 is an oral protease-activated receptor 4 (PAR4) inhibitor that was being developed for arterial thrombosis. PAR4 was long considered a redundant “backup” receptor to the more popular and well-researched PAR1 receptor, owing in part to the higher thrombin levels required for activation and the slower signaling response the receptor induces. However, a new hypothesis, also espoused by BMS scientists in developing BMS-986120, suggests that targeting PAR4 may offer an improved window between antithrombotic efficacy and bleeding time due to its signaling kinetics. Given its role in sustained thrombin signaling, blocking PAR4 is expected to preclude unwanted stable thrombus growth, while transient signaling through PAR1 is left untouched to preserve initial thrombus formation. Preclinical data seem to lend support…

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