Few areas in cardiovascular pharmacotherapy are still progressing at a considerable pace. While vitamin-K antagonists have been used for decades, their safety problems are of essential concern, and only recently genetic methods have been successfully employed (CYP 2C9 and VKOR polymorphisms) to tailor dosing and, thus, promote personalized medicine in this area. Being major drivers of innovation in this field, novel oral anticoagulants have been approved recently, the factor Xa inhibitor rivaroxaban and the factor Ila inhibitor dagibatran after the earlier failure of ximelagatran due to liver toxicity; apixaban, betrixaban, and YM 150 are in advanced clinical development. Their proposed advantages over coumadins are fixed dosage, lack of routine monitoring of coagulation values, less drug-drug interactions and drug-food-interactions. Though initially only indicated for thrombosis prevention in surgical procedures, large trials are ongoing or have been recently finished to position those drugs in atrial fibrillation and unstable angina treatment. While these compounds will represent a jump innovation and allow for anticoagulation even in elderly patients ineligible for warfarin therapy, progress regarding parenteral anticoagulants (conventional and low molecular weight heparins), is better described as step innovation. Fondaparinux has favourable efficacy and safety data as compared to older low molecular weight heparins. Idrabiotraparinux can be antagonized by avidin, and is currently investigated in patients suffering from acute venous thromboembolism or atrial fibrillation. Idraparinux was terminated due to major bleeding complications.
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