Bivalirudin

Bivalirudin is an inhibitor of α- and ζ-thrombin (K_is = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.¹ It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM.² Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner.³ Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.⁴

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1. Witting, J.I., Bourdon, P., Brezniak, D.V., et al. Thrombin-specific inhibition by and slow cleavage of hirulog-1. Biochem J. 283(Pt 3), 737-743 (1992).

2. Ofosu, F.A., Fenton, J.W., II, Maraganore, J.M., et al. Inhibition of the amplification reactions of blood coagulation by site-specific inhibitors of α-thrombin. Biochem J. 283(Pt 3), 893-897 (1992).

3. Hamelink, J.K., Tang, D.B., Barr, C.F., et al. Inhibition of platelet deposition by combined hirulog and aspirin in a rat carotid endarterectomy model. J. Vasc. Surg. 21(3), 492-498 (1995).

4. Shah, P.B., Ahmed, W.H., Ganz, P., et al. Bivalirudin compared with heparin during coronary angioplasty for thrombus-containing lesions. J. Am. Coll. Cardiol. 30(5), 1264-1269 (1997).