Bivalirudin: a review.
Bivalirudin (Angiomax) is a thrombin-inhibiting oligopeptide that was developed via rational drug design as a hirudin analogue ('hirulog'). Similar to hirudin, it is a bivalent thrombin inhibitor, as its 20-amino acid structure combines a carboxy-terminal region that recognises thrombin's fibrin(ogen)-binding site, and an amino-terminal tetrapeptide that inhibits the active site of thrombin, connected by a tetraglycine spacer. It has certain pharmacological advantages over hirudin, including enzymic metabolism (less dependence on renal clearance) and low immunogenicity (reduced potential for anaphylaxis). Bivalirudin is approved for use in percutaneous transluminal coronary angioplasty (PTCA), and is undergoing active investigation for anticoagulation during cardiac surgery, both 'off-pump' and with cardiopulmonary bypass ('on-pump'). Anecdotal 'off-label' experience for the treatment of heparin-induced thrombocytopenia shows promise.
Warkentin
Theodore E
TE
Department of Pathology and Molecular Medicine, McMaster University, Hamilton, Ontario, Canada. twarken@mcmaster.ca
Koster
Andreas
A
D000595:Amino Acid Sequence / Q000235:genetics; D015906:Angioplasty, Balloon, Coronary; D000818:Animals; D000925:Anticoagulants / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000991:Antithrombins / Q000235:genetics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006629:Hirudins / Q000235:genetics / Q000493:pharmacokinetics; D006801:Humans; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000235:genetics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011994:Recombinant Proteins / Q000235:genetics / Q000493:pharmacokinetics / Q000627:therapeutic use
D000925:Anticoagulants; D000991:Antithrombins; D006629:Hirudins; D010446:Peptide Fragments; D011994:Recombinant Proteins; C074619:bivalirudin