Idraparinux and idrabiotaparinux

Abstract

Idraparinux is a polymethylated synthetic pentasaccharide that binds to antithrombin with high affinity. Idrabiotaparinux is a derivative of idraparinux with biotin synthesized to the end-standing hexose. This article reports on data carried out with both compounds until April 2009. Idraparinux once weekly 2.5 mg subcutaneous was almost as effective for treatment of deep vein thrombosis but less effective for pulmonary embolism as initial bodyweight-adjusted subcutaneous enoxaparin followed by international normalized ratio-adjusted warfarin over 6 months for prophylaxis of recurrent venous thromboembolism (VTE). Prolonged prophylaxis of recurrent VTE with idraparinux was more effective but induced severe bleedings compared with placebo over an additional 6 months of prophylaxis of recurrent VTE. Prophylaxis of embolic events with idraparinux over an 18-month period in patients with atrial fibrillation was as effective as international normalized ratio-adjusted warfarin but induced more major bleeding complications. The elimination half-life of idraparinux increased to 60 days in these studies, which may explain the bleeding complications. As such the development of idraparinux was stopped. Idrabiotaparinux is eliminated after intravenous administration of avidin. Currently idrabiotaparinux once weekly 3.5 mg subcutaneous is being investigated in clinical trials for the prevention of recurrent events in patients with acute VTE and atrial fibrillation. The future of idrabiotaparinux depends on the demonstration of its safety and efficacy. Avidin also has to demonstrate its efficacy and safety after single and repeated injections.

Keywords::

• atrial fibrillation
• idrabiotaparinux
• idraparinux
• thrombosis

Financial & competing interests disclosure

The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.