Pharmacokinetic and pharmacodynamic modeling and simulation analysis of CTB-001, a recently developed generic of bivalirudin
PK/PD study published in Pharmaceutical Research (2019)
Abstract
PURPOSE: CTB-001, a recently developed generic version of bivalirudin, an FDA-approved anticoagulant used for prophylaxis and treatment of cardiovascular diseases, has shown good efficacy and safety in clinical trials. We characterized the pharmacokinetics (PK) and pharmacodynamics (PD) of CTB-001 by modeling and simulation analysis. METHODS: PK/PD data were collected from a randomized, double-blind, placebo-controlled, single-dose, dose-escalation phase 1 study conducted in 24 healthy Korean male subjects. PK/PD analysis was conducted sequentially by nonlinear mixed-effects modeling implemented in NONMEM®. Monte-Carlo simulations were conducted for PK, activated partial thromboplastin time (aPTT), prothrombin time (PT), and thrombin time (TT). RESULTS: The CTB-101 PK was best described by a three-compartment linear model with a saturable binding peripheral compartment. All PD endpoints showed dose-response relationship, and their changes over time paralleled those of CTB-101 concentrations. A simple maximum effect model best described the aPTT, PT in INR, PT in seconds, and TT, whereas an inhibitory simple maximum effect model best described PT in percentages. The maximum duration of effect of CTB-001 on aPTT prolongation was 52.1 s. CONCLUSIONS: The modeling and simulation analysis well-characterized the PK and PD of CTB-001 in healthy Koreans, which will be valuable for identifying optimal dosing regimens of CBT-001.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
PK/PD modeling of CTB-001 generic bivalirudin demonstrating bioequivalence to reference formulation with predictable ACT response across body weights.
Por qué esto importa para la hirudoterapia
Este estudio caracterizó la farmacocinética y la farmacodinamia de CTB-001, descrito en el resumen como una versión genérica recientemente desarrollada de bivalirudina (un anticoagulante aprobado por la FDA), mediante modelado y simulación utilizando datos de un estudio de fase 1 en dosis única, aleatorizado, doble ciego y controlado con placebo, en 24 varones coreanos sanos. La FC de CTB-001 se describió mejor mediante un modelo lineal de tres compartimentos con unión periférica saturable; todos los desenlaces de FD mostraron relación dosis-respuesta, con una duración máxima del efecto sobre la prolongación del aPTT de 52,1 s. El resumen no menciona la hirudina, las sanguijuelas ni ningún origen derivado de sanguijuelas. ADVERTENCIA: este resumen no establece ninguna conexión con la hirudoterapia ni con el secretoma de la sanguijuela; la relevancia con el ámbito de la ASH no está respaldada.
Citación
Pharmacokinetic and pharmacodynamic modeling and simulation analysis of CTB-001, a recently developed generic of bivalirudin.
Han S et al. · Pharmaceutical research, 2019
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026