Direct thrombin inhibitors: patents 2002-2012
Review published in Mol Med Rep (2014)
Abstract
Acute vascular diseases and other thromboses of the blood system constitute major health risks in developing countries. Thrombin plays a central role in blood coagulation, which is a crucial process involved in thrombosis. Direct thrombin inhibitors (DTIs) such as argatroban, dabigatran, dabigatran etexilate, lepirudin, desirudin and bivalirudin, which bind to thrombin and block its enzymatic activity, are widely and effectively used in the treatment of thromboembolic diseases. DTIs appear to overcome the disadvantages of indirect thrombin inhibitors such as unfractionated heparins (UFH). Although these DTIs show specific advantages over indirect inhibitors, they still present limitations, such as a narrow therapeutic window, and bleeding and anaphylaxis as side-effects. Novel anticoagulant drugs need thus to be developed to overcome these limitations. In the search for additional candidate agents with improved efficacy, safety and high bioavailability in oral administration, a high number of compounds has been identified, such as those derived from the tripeptide template D-Phe-Pro-Arg, aptamers and peptides isolated from blood-sucking animals. These candidates may prove the new agents of choice for the treatment of cardiovascular diseases.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Patent-focused review (2002-2012) of direct thrombin inhibitors — leech-derived hirudins, bivalirudin, lepirudin, desirudin, dabigatran. Documents D-Phe-Pro-Arg tripeptide derivatives, aptamers, and peptides from blood-feeding animals as candidate scaffolds.
Por qué esto importa para la hirudoterapia
Esta revisión analiza los inhibidores directos de la trombina (IDT), entre ellos argatrobán, dabigatrán, dabigatrán etexilato, lepirudina, desirudina y bivalirudina, y su uso en el tratamiento de enfermedades tromboembólicas. Los autores señalan las limitaciones de los IDT —estrecha ventana terapéutica, hemorragia y anafilaxia— e identifican nuevos compuestos candidatos, incluidos los derivados de plantillas tripeptídicas, aptámeros y péptidos aislados de animales hematófagos, como posibles anticoagulantes de próxima generación. Para el ámbito de la ASH, la relevancia es indirecta: el resumen menciona a los animales hematófagos como fuente de nuevos candidatos a fármacos anticoagulantes, lo que podría abarcar moléculas derivadas de sanguijuelas, aunque no se nombra específicamente a las sanguijuelas. Advertencia: se trata de una revisión sin datos experimentales originales sobre sanguijuelas o hirudoterapia; el resumen no menciona específicamente a las sanguijuelas, la hirudina ni la terapia con sanguijuelas, y la conexión con la biología de las sanguijuelas es inferencial.
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026