Title: Bivalirudin
CAS Registry Number: 128270-60-0
Synonyms: Hirulog-1; hirulog-8
Manufacturers' Codes: BG-8967
Trademarks: Angiomax (Medicines Co.); Angiox (Nycomed); Hirulog (Medicines Co.)
Molecular Formula: C98H138N24O33
Molecular Weight: 2180.29
Percent Composition: C 53.99%, H 6.38%, N 15.42%, O 24.22%
Literature References: Synthetic peptide of 20 amino acids; member of a novel class of bivalent direct thrombin inhibitors. 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). Clinical study in myocardial infarction: P. Théroux
et al., Circulation 91, 2132 (1995); during coronary angioplasty: J. A. Bittl
et al., N. Engl. J. Med. 333, 764 (1995). Clinical trial with provisional glycoprotein IIb/IIIa inhibition during percutaneous coronary intervention: A. M. Lincoff
et al., J. Am. Med. Assoc. 289, 853 (2003). Review of pharmacology and clinical development: T. D. Gladwell,
Clin. Ther. 24, 38-58 (2002); of clinical experience in acute coronary syndromes: J. S. Kalus, M. F. Caron,
Expert Opin. Invest. Drugs 13, 465-477 (2004).
Therap-Cat: Antithrombotic.
Keywords: Antithrombotic; Anticoagulant.
