Bivalirudin Pathway


Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.

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References

  1. Jennings, L.K., & Saucedo, J.F. (2008). Antiplatelet and anticoagulant agents: key differences in mechanisms of action, clinical application, and therapeutic benefit in patients with non-ST-segment-elevation acute coronary syndromes. Current Opinion in Cardiology, 23(4), 302-308. PMID: 18520712
  2. Walker, C.P., & Royston, D. (2002). Thrombin generation and its inhibition: a review of the scientific basis and mechanism of action of anticoagulant therapies. British Journal of Anaesthesia, 88(6), 848-863. PMID: 12173205