Betrixaban

Betrixaban is an inhibitor of the serine protease Factor Xa (K_i = 0.117 nM; IC₅₀ = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.¹ It is selective for Factor Xa over hERG channels (K_i = 1.8 µM; IC₅₀ = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.² In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.³

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1. Zhang, P., Huang, W., Wang, L., et al. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg. Med. Chem. Lett. 19(8), 2179-2185 (2009).

2. Chan, N.C., Bhagirath, V., and Eikelboom, J.W. Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc. Health Risk Manag. 11, 343-351 (2015).

3. Cohen, A.T., Harrington, R., Goldhaber, S.Z., et al. The design and rationale for the acute medically Ill venous thromboembolism prevention with extended duration betrixaban (APEX) study. 167(3) 335-341 (2014).