Ximelagatran--a promising new drug in thromboembolic disorders.
Research article published in Current pharmaceutical design (2005)
Abstract
Ximelagatran is an oral direct thrombin inhibitor (DTI), the active form of which is melagatran. Approximately 20% of an oral ximelagatran dose becomes bioavailable as melagatran, which binds noncovalently and reversibly to both fibrin-bound and freely circulating thrombin. Oral ximelagatran dosing not only inhibits thrombin activity rapidly, competitively, and potently, but also delays and suppresses thrombin generation. In humans, oral ximelagatran exhibits anticoagulant, antiplatelet, and profibrinolytic effects, with only minor prolongation of the capillary bleeding time. Oral ximelagatran exhibits a stable and predictable pharmacokinetic profile during repeated dosing, with low intra- and inter-individual variation, and a low potential for interaction with other medications. It is excreted primarily as melagatran via the kidney, without unexpected bioaccumulation. Dosing requirements do not vary with age, gender, ethnicity, obesity, or food or alcohol intake. Clinical trials (total n>30,000) have evaluated oral ximelagatran in four indications: the prevention of venous thromboembolism (VTE, comprising deep venous thrombosis with or without and pulmonary embolism) after elective hip- or knee-replacement surgery (with approval granted by France, as the Reference Member State for the European Union); treatment and long-term secondary prevention of VTE; the prevention of stroke and other systemic embolic events associated with nonvalvular atrial fibrillation; and the prevention of cardiovascular events after an acute myocardial infarction. The results of these trials suggest that the benefit-risk profile of oral ximelagatran therapy, administered at a fixed-dose without coagulation monitoring, compares favorably with that of currently approved standard therapy.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Ximelagatran--a promising new drug in thromboembolic disorders.
Por qué esto importa para la hirudoterapia
Esta revisión describe el ximelagatrán, un inhibidor directo de la trombina por vía oral cuya forma activa (melagatrán) se une de forma no covalente y reversible tanto a la trombina unida a fibrina como a la circulante libre, con una biodisponibilidad oral aproximada del 20 % y una farmacocinética estable y predecible. Los ensayos clínicos que incluyeron a más de 30 000 pacientes evaluaron el ximelagatrán para la prevención del tromboembolismo venoso tras reemplazo de cadera o rodilla, el tratamiento y la prevención secundaria del TEV, la prevención del accidente cerebrovascular en la fibrilación auricular no valvular, y la prevención de eventos cardiovasculares tras infarto agudo de miocardio, con un perfil beneficio-riesgo favorable a dosis fijas sin monitorización de la coagulación. Si bien el ximelagatrán es un inhibidor directo de la trombina —la misma clase farmacológica amplia que la hirudina—, se trata de un compuesto totalmente sintético sin conexión alguna con las sanguijuelas, el secretoma de las sanguijuelas ni la hirudoterapia. Este artículo no tiene una relevancia defendible para el ámbito de la ASH.
Citación
Ximelagatran--a promising new drug in thromboembolic disorders.
Petersen · Current pharmaceutical design, 2005
Contexto clínico relacionado
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Añadido a la biblioteca ASH: May 28, 2026 · Última actualización del sitio: June 18, 2026