Past, present and future of hirudin
Basic science / preclinical published in Haemostasis (1991)
Abstract
The naturally occurring anticoagulant from medicinal leeches, hirudin, which we isolated and biochemically analyzed 30 years ago as a miniprotein with specific antithrombin activity, has afterwards been employed for scientific and diagnostic purposes in hematology. Pure hirudin proved to be an antithrombotic agent of high quality that displays an antithrombotic action dependent upon its blood level. After intravenous injection, it is distributed in the extracellular space and is almost completely eliminated through the kidneys by glomerular filtration in a biologically active form. The efficacy of hirudin in preventing venous and arterial thrombosis and disseminated intravascular coagulation was demonstrated in various animal models. Clinical pharmacological studies corroborated the specific pharmacodynamic and pharmacokinetic properties of hirudin found in animal experiments. Genetic engineering led to the availability of sufficient quantities of recombinant hirudin (r-hirudin) for clinical purposes. Pharmacologic profiling of r-hirudin showed that both its pharmacokinetic and pharmacodynamic characteristics are very similar to those of native hirudin. Clinical pharmacological studies with r-hirudin revealed that, at single therapeutically relevant doses, r-hirudin is a well-tolerated and potent anticoagulant without any detectable side effects and allergic reactions. Further preclinical studies of r-hirudin should concentrate on identifying possible indications for use, on the development of r-hirudin preparations and derivatives, and on the development of antidotes for hirudin.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
The naturally occurring anticoagulant from medicinal leeches, hirudin, which we isolated and biochemically analyzed 30 years ago as a miniprotein with specific antithrombin activity, has afterwards been employed for scientific and diagnostic purposes in hematology.
Por qué esto importa para la hirudoterapia
Este artículo traza el desarrollo científico de la hirudina —el anticoagulante natural aislado de las sanguijuelas medicinales— desde su caracterización bioquímica como una miniproteína antitrombina específica hasta la producción y evaluación farmacológica de la hirudina recombinante (r-hirudina). El resumen informa que la acción antitrombótica de la hirudina depende de su nivel sanguíneo, que se distribuye en el espacio extracelular y se elimina a través de los riñones, y que su eficacia en la prevención de la trombosis venosa y arterial y de la coagulación intravascular diseminada se demostró en modelos animales; la r-hirudina se describe como poseedora de propiedades farmacocinéticas y farmacodinámicas similares a las de la hirudina nativa y como un anticoagulante potente y bien tolerado a dosis únicas terapéuticamente relevantes en estudios de farmacología clínica. Este trabajo es central para el ámbito de ASH porque la hirudina es el anticoagulante principal derivado de las sanguijuelas medicinales, y su caracterización farmacológica informa directamente la terapia basada en sanguijuelas y el desarrollo de fármacos derivados de sanguijuelas. El resumen ofrece una revisión amplia de varias décadas en lugar de resultados cuantitativos detallados de un único estudio, y no se presentan datos de resultados clínicos a gran escala.
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Añadido a la biblioteca ASH: March 18, 2026 · Última actualización del sitio: June 18, 2026