Pentasaccharide Derivatives
The pivotal position of factor Xa in the coagulation cascade has made its inhibition an attractive target for therapy in the setting of venous thromboembolic events and coronary thrombosis. This chapter explores the mechanism of antithrombotic action of fondaparinux (a pentasaccharide) and reviews clinical trials with fondaparinux and its derivatives in venous and arterial thromboembolic diseases. Based on current evidence fondaparinux 2.5 mg SC daily is currently approved for deep vein thrombosis (DVT) prophylaxis in patients undergoing surgery for hip fracture or replacement, knee replacement and thromboembolism following abdominal surgery. Fondaparinux is approved for treatment of patients with pulmonary embolus or DVT in the setting of warfarin therapy bridging. The management of non-ST segment elevation (NSTE)-ACS with fondaparinux is supported by a Class I recommendation from both the American College of Cardiology/American Heart Association (ACC/AHA) and the European Society of Cardiology (ESC). In patients undergoing an early invasive strategy, the addition of a second anticoagulant with anti-factor IIa activity during percutaneous coronary intervention (PCI) is recommended by both the ACC/AHA and ESC. New synthetic long-acting reversible parenteral pentasaccharides are currently under study. © 2013 Blackwell Publishing Ltd.