Focus on ximelagatran: A new oral anticoagulant

Although warfarin is an effective drug in the treatment and prevention of thromboembolism, dosing complexities and drug interactions have led to its underutilization and a desire for an alternative agent. Ximelagatran (Exanta, AstraZeneca) is a novel oral anticoagulant that can be taken in standardized doses without the use of periodic blood monitoring to determine the level of anticoagulation. Large prospective clinical trials have shown ximelagatran to be similar in efficacy compared to the standard of therapy in the prevention and treatment of thromboembolism with similar or lower rates of bleed. Of concern, however, is the fact that that ximelagatran may elevate hepatic enzymes. An NDA was filed for ximelagatran on December 23, 2003, and FDA’s Cardiovascular and Renal Drugs Advisory Committee is scheduled to review the drug for the prevention of stroke and thromboembolism at a meeting on September 10, 2004. This article reviews ximelagatran’s chemistry and pharmacology, pharmacokinetics, clinical trials, adverse effects, drug interactions, and dosage and administration.