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
This review discusses direct thrombin inhibitors (DTIs) including argatroban, dabigatran, dabigatran etexilate, lepirudin, desirudin, and bivalirudin, and their use in treating thromboembolic diseases. The authors note DTIs' limitations — narrow therapeutic window, bleeding, and anaphylaxis — and identify novel candidate compounds, including those derived from tripeptide templates, aptamers, and peptides isolated from blood-sucking animals, as potential next-generation anticoagulant agents. For ASH's domain, the relevance is indirect: the abstract mentions blood-sucking animals as a source for new anticoagulant drug leads, which could encompass leech-derived molecules, though leeches are not specifically named. Caveat: this is a review with no original experimental data on leeches or hirudotherapy; the abstract does not specifically mention leeches, hirudin, or leech therapy, and the connection to leech biology is inferential.
Citación
Contexto clínico relacionado
Explore cómo esta investigación se conecta con la práctica clínica
Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: June 18, 2026