GSK2981278

GSK2981278 is a potent, selective, and reversible small molecule inhibitor of coagulation Factor XIa (FXIa). Developed by GSK, it was designed as an antithrombotic agent to prevent venous thromboembolism (VTE) with a reduced risk of bleeding compared to conventional anticoagulants that target the common pathway of coagulation. By targeting FXIa, the compound inhibits the intrinsic pathway of the coagulation cascade, which is thought to be more critical for pathological thrombus formation than for physiological hemostasis. Clinical development reached Phase 2 for the prevention of VTE in patients undergoing total knee arthroplasty; however, the program was subsequently discontinued by the sponsor.

Other names

N(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamide