Safety, tolerability, pharmacodynamics, and pharmacokinetics of recombinant Neorudin, a new anticoagulant drug, in patients undergoing coronary angiography
Phase II study published in Clinical Pharmacology in Drug Development (2024)
Abstract
This study evaluated the safety, tolerability, pharmacodynamics, and pharmacokinetics of recombinant neorudin (EPR-hirudin [EH]) in patients with acute coronary syndrome (ACS), providing a basis for further therapeutic research. This open-label, single-center, nonrandomized, nonblinded, and noncontrolled trial categorized 24 patients with nonprogressive ACS who met the screening criteria into 3 groups. They received an intravenous injection of neorudin (0.4 mg/kg), followed by an intravenous drip at doses of 0.15, 0.30, and 0.45 mg/kg/h for 3 days in the low-, medium-, and high-dose groups, respectively. The safety, tolerability, pharmacodynamics, and pharmacokinetics of EH were assessed after treatment, indicating that neorudin was safe and well tolerated in nonprogressive ACS. No serious adverse events or clinical composite end points were observed. The activated partial thromboplastin time and thrombin time increased significantly and dose dependently following EH administration across all groups compared to pretreatment values. Conversely, thrombin activity significantly decreased after drug administration but returned to baseline levels shortly after drug withdrawal. Within the administered dose range, neorudin exposure increased with the dose, and its half-life was approximately 2 hours. Neorudin was found to be safe and tolerable for treating patients with nonprogressive ACS, demonstrating therapeutic efficacy at doses up to 0.45 mg/kg/h over a 3-day period.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Phase II clinical study of recombinant neorudin in coronary angiography patients. Linear pharmacokinetics, dose-dependent aPTT prolongation, favorable safety profile.
Por qué esto importa para la hirudoterapia
Este ensayo abierto, unicéntrico, no aleatorizado, no enmascarado y no controlado evaluó la seguridad, la tolerabilidad, la farmacodinámica y la farmacocinética de la neorudina recombinante (EPR-hirudina), un inhibidor directo de la trombina basado en la hirudina, en 24 pacientes con síndrome coronario agudo no progresivo distribuidos en tres grupos de dosis (infusión de 0,15, 0,30 y 0,45 mg/kg/h durante 3 días tras un bolo de 0,4 mg/kg). La neorudina se notificó como segura y bien tolerada, sin acontecimientos adversos graves ni criterios de valoración clínicos compuestos, y produjo aumentos dependientes de la dosis del tiempo de tromboplastina parcial activada y del tiempo de trombina, redujo la actividad de la trombina, mostró una vida media de aproximadamente 2 horas y una exposición proporcional a la dosis. Dado que la neorudina es un derivado recombinante de la hirudina —el anticoagulante segregado por las sanguijuelas medicinales—, estos datos farmacológicos de fase temprana son relevantes para los miembros de la ASH que siguen la traslación clínica de los terapéuticos derivados del secretoma de la sanguijuela. La advertencia clave es que se trató de un estudio pequeño, no controlado y abierto sin brazo comparador, por lo que respalda la realización de más investigaciones en lugar de establecer una eficacia definitiva.
Citación
Safety, tolerability, pharmacodynamics, and pharmacokinetics of recombinant Neorudin, a new anticoagulant drug, in patients undergoing coronary angiography.
Liu YB et al. · Clinical pharmacology in drug development, 2024
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: 18 de junio de 2026