bms-986177

Milvexian (BMS-986177/JNJ-70033093) is an orally bioavailable, small-molecule, reversible, and direct antagonist of Factor XIa (FXIa). It exhibits potent inhibitory activity across species, with Ki values of 0.11 nM for human, 0.38 nM for rabbit, and 0.64 nM for dog. By targeting FXIa, Milvexian selectively inhibits the intrinsic pathway of the coagulation cascade. It demonstrates robust antithrombotic efficacy in various in vitro and in vivo models while maintaining a favorable safety profile regarding bleeding risk. It is a critical tool for investigating novel anticoagulant strategies in thrombosis and cardiovascular research.

UAWJ-247 is a SARS-CoV-2 Main Protease inhibitor (IC50 = 45 nM).

Milvexian, also known as BMS-986177 and JNJ-70033093, is a blood coagulation factor XIa inhibitor. Milvexian demonstrated good selectivity over plasma kallikreinKi = 44 nM (400-fold selective), and chymotrypsinKi = 35 nM (318-fold selective). At a dose of 1.5 mg/kg, Milvexian exhibited an overall exposure of 1215 nM/h, low clearance of 10.3 mL/min/kg, and oral bioavailability of 32%.