1310. Bivalirudin

Description and references

Synthetic peptide of 20 amino acids; a specific and reversible bivalent direct thrombin inhibitor. Characterized by an anion binding exosite (ABE) derived from hirudin, q.v., linked to a thrombin catalytic site inhibitor moiety by tetraglycine. Prepn and structure activity study: J. M. Maraganore et al., WO 9102750; eidem, US 5196404 (1991, 1993 both to Biogen); eidem, Biochemistry 29, 7095 (1990). Determn in plasma and whole blood: T. J. Reid, B. M. Alving, Thromb. Haemostasis 70, 608 (1993). Clinical pharmacology: I. Fox et al., ibid. 69, 157 (1993). Review of pharmacology and clinical development: N. W. Shammas, Cardiovasc. Drug Rev. 23, 345-360 (2005); of clinical experience in coronary syndromes: T. E. Warkentin, A. Koster, Expert Opin. Pharmacother. 6, 1349-1371 (2005).