jnj-70033093

Milvexian (BMS-986177) 是一种具有口服生物利用度、小分子、可逆且直接的 凝血因子 XIa (Factor XIa) 拮抗剂。它对人类 FXIa 表现出极高的亲和力 (Ki = 0.11 nM)，并对兔、狗、大鼠和小鼠的 FXIa 也具有显著的选择性抑制作用。作为一种新型抗凝药物，Milvexian 通过阻断内源性凝血途径的关键环节发挥抗血栓活性，同时在临床前研究中显示出比传统抗凝剂更低的出血风险，常用于血栓形成、卒中预防以及大手术后静脉血栓栓塞的研究。

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%.