New anticoagulants - direct thrombin inhibitors
Review published in Therapeutische Umschau (2012)
Abstract
Direct thrombin-inhibitors inactivate not only free but also fibrin-bound thrombin. The group of parenteral direct thrombin-inhibitors includes the recombinant hirudins lepirudin and desirudin, the synthetic hirudin bivalirudin, and the small molecule argatroban. All these compounds do not interact with PF4/heparin-antibodies. Therefore, argatroban as well as bivalirudin are currently used to treat heparin-induced thrombocytopenia (HIT). The oral direct thrombin-inhibitor dabigatran etexilate is already licensed in many countries for the treatment of non-valvular atrial fibrillation. Dabigatran etexilate reveals a stable and predictable effect that allows a medication without dose adjustment or monitoring. The substance shows only few interactions with other drugs but strong inhibitors of p-glycoprotein can increase plasma levels of dabigatran substantially. After oral intake, the prodrug dabigatran etexilate is cleaved by esterase-mediated hydrolyses to the active compound dabigatran. Elimination of dabigatran is predominantly renal. Safety and efficacy of dabigatran etexilate were tested in an extensive clinical study program. Non-inferiority compared to current standard treatments was shown for prophylaxis of venous thromboembolic events after total knee and hip replacement, for stroke prevention in atrial fibrillation, and for treatment of acute venous thromboembolism. In daily practice, Dabigatran etexilate competes against the new direct factor Xa-inhibitors. In the absence of direct comparative clinical trials, it is not yet clear if one class of substances has distinct advantages over the other.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Review of parenteral (lepirudin, desirudin, bivalirudin, argatroban) and oral (dabigatran etexilate) direct thrombin inhibitors covering use in HIT, atrial fibrillation, and venous thromboembolism.
Por qué esto importa para la hirudoterapia
Esta revisión farmacológica examina los inhibidores directos de la trombina, incluidas las hirudinas recombinantes lepirudina y desirudina, la hirudina sintética bivalirudina, el argatroban y el agente oral dabigatrán etexilato, analizando sus mecanismos y aplicaciones clínicas en la trombocitopenia inducida por heparina y la profilaxis tromboembólica. Para ASH y la hirudoterapia, este artículo es directamente relevante porque la lepirudina, la desirudina y la bivalirudina se derivan de la hirudina o están modeladas a partir de ella, el anticoagulante distintivo del secretoma de la sanguijuela medicinal, y la revisión describe sus propiedades farmacológicas establecidas y sus funciones clínicas como agentes antitrombóticos. El artículo aporta un contexto útil sobre cómo encajan las terapias anticoagulantes derivadas de la sanguijuela en el panorama más amplio de la inhibición de la trombina, incluida su ventaja de no interactuar con los anticuerpos contra PF4/heparina. No obstante, como revisión narrativa, sintetiza la literatura existente en lugar de presentar nuevos datos de ensayos, y la disponibilidad clínica de algunos agentes puede haber cambiado desde la publicación.
Citación
Contexto clínico relacionado
Explore cómo esta investigación se conecta con la práctica clínica
Añadido a la biblioteca ASH: May 26, 2026 · Última actualización del sitio: 18 de junio de 2026