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Recombinant Hirudin Antigen for PK/PD Studies

Hirudin prevents or dissolves the formation of clots and thrombi, and has therapeutic value in blood coagulation disorders, in the treatment of skin hematomas and of superficial varicose veins. Recombinant hirudin (r-hirudin or lepirudin) not only provides effective anticoagulation in patients with heparin-induced thrombocytopenia (HIT) but also allows rapid platelet recovery. The quantification of r-hirudin is very important for pharmacokinetics (PK) and pharmacodynamics (PD) studies of r-hirudin especially. It is used also for monitoring r-hirudin concentrations in the clinical laboratory for diagnostic purposes. Therefore, Creative Diagnostics has developed recombinant hirudin that is suitable for in vitro laboratory research application where an efficient inhibition of thrombin is required.

Highlight Features

  • Excellent biological activity (Specific activity >13,000 ATU/mg by chromogenic assay)
  • Purified by proprietary chromatographic techniques (Purity > 95% by RP-HPLC analyses)
  • Provided as lyophilized (Shelf life: 3 years)
  • Recombinant hirudin are in stock and can be manufactured in bulk quantities
Cat. No DAG3450
Product Name Recombinant H. medicinalis Hirudin
Host Pichia pastoris
Molecular Weight 7 kDa
Specific Activity 13,000 ATU/mg
Purity >95% by RP-HPLC
Format White lyophilized powder
Storage 2-8°C for short term, -20°C for long term

Background

The chemical structure of natural hirudin

Fig. 1 The chemical structure of natural hirudin

Natural hirudin is a polypeptide isolated from the salivary glands of the Hirudo medicinalis, which is composed of 64-66 amino acids with a molecular weight of about 7 KDa. However, the low production of natural hirudin limits its research and application. Recombinant hirudin (r-hirudin or lepirudin) is a direct irreversible thrombin inhibitor by binding to both free and clot-bound thrombin. It is approved for treatment of heparin-induced thrombocytopenia (HIT), which is a serious antibody-mediated drug reaction mostly associated with the use of unfractionated heparin. Clinical experience during the last 10 years has proved the efficacy of lepirudin in the management of HIT. The major route of elimination of lepirudin is the kidney, an elimination half-life of 60 to 100 minutes, a mean total clearance of 170 to 190 ml/min. In HIT patients, lepirudin is given to avoid clot formation, but at the same time the risk of bleeding has to be minimized. The risk of bleeding can be reduced by implementing an optimal monitoring and dose adjustment strategy, particularly in patients undergoing cardiopulmonary bypass surgery and in those with impaired renal function.

References

  1. Petros S. (2008). Lepirudin in the management of patients with heparin-induced thrombocytopenia. Biologics. 2(3), 481-490.
  2. Kiser T H, Jung R, Maclaren R, et al. (2005). Evaluation of diagnostic tests and argatroban or lepirudin therapy in patients with suspected heparin-induced thrombocytopenia. Pharmacotherapy the Journal of Human Pharmacology & Drug Therapy. 25(12), 1736-1745.
  3. Fischer K G, Loo A V D, Bhler J. (1999). Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Clinical Trials. 72, S46-50.
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