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.
Summary
Phase II clinical study of recombinant neorudin in coronary angiography patients. Linear pharmacokinetics, dose-dependent aPTT prolongation, favorable safety profile.
Why This Matters for Hirudotherapy
This open-label, single-center, nonrandomized, nonblinded, noncontrolled trial evaluated the safety, tolerability, pharmacodynamics, and pharmacokinetics of recombinant neorudin (EPR-hirudin), a hirudin-based direct thrombin inhibitor, in 24 patients with nonprogressive acute coronary syndrome across three dose groups (0.15, 0.30, and 0.45 mg/kg/h infusion over 3 days following a 0.4 mg/kg bolus). Neorudin was reported as safe and well tolerated, with no serious adverse events or composite clinical end points, and produced dose-dependent increases in activated partial thromboplastin time and thrombin time, reduced thrombin activity, an approximately 2-hour half-life, and dose-proportional exposure. Because neorudin is a recombinant derivative of hirudin — the anticoagulant secreted by medicinal leeches — these early-phase pharmacologic data are relevant to ASH members who follow the clinical translation of leech-secretome therapeutics. The key caveat is that this was a small, uncontrolled, open-label study without a comparator arm, so it supports further investigation rather than establishing definitive efficacy.
Citation
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
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