Current anticoagulants

Vitamin K antagonists and heparins have dominated the anticoagulant market for over half a century. Warfarin inhibits the vitamin K-dependent activation of several clotting factors (Fig. 1) and is the most commonly prescribed anticoagulant. Until recently, it was the only orally bioavailable agent of this kind and it remains the only approved drug for long-term anticoagulation therapy. Use of warfarin in patients with atrial fibrillation reduces the incidence of stroke by 64%. Despite proven efficacy, warfarin carries the risk of serious or fatal bleeding, has an unpredictable pharmacokinetic profile, is subject to drug–drug interactions and is affected by an individual's genetic make-up and diet, making it hard to dose. Various generic vitamin K antagonists overall generated global sales of over US$700 million in 2008 (Ref. 2).

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