Bivalirudin: a review
Review published in Expert Opinion on Pharmacotherapy (2005)
Abstract
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.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Резюме
Bivalirudin, a synthetic 20-amino acid hirudin analog (hirulog), is reviewed as a bivalent thrombin inhibitor with enzymatic metabolism, low immunogenicity, and FDA approval for percutaneous coronary intervention.
Почему это важно для гирудотерапии
This review describes bivalirudin, a thrombin-inhibiting oligopeptide developed through rational drug design as a hirudin analogue ('hirulog'), covering its bivalent 20-amino acid structure, pharmacological advantages over hirudin (including enzymic metabolism and low immunogenicity), approved clinical use in percutaneous transluminal coronary angioplasty, and investigational applications in cardiac surgery and heparin-induced thrombocytopenia. Its relevance to the ASH domain is indirect: the abstract discusses bivalirudin explicitly in relation to hirudin, illustrating how hirudin-like bivalent thrombin inhibition has been pharmacologically refined for a clinically approved anticoagulant. However, the abstract makes no reference to leeches, leech saliva, or hirudotherapy, and as a review it provides no original experimental or clinical data, so its connection to hirudotherapy is limited to the shared pharmacological framework of hirudin-related thrombin inhibition.
Цитирование
Связанный клинический контекст
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