About this Pharmacology, Toxicology and Pharmaceutics article
Safety, pharmacokinetics and exploratory exposure-response analysis of CX3002, a novel inhibitor of Xa, in Chinese healthy subjects by Wenjun Chen; Zourong Ruan; Honggang Lou; Lu Wang; Rong Shao; Fenghua Li; Bo Jiang is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
Background and objective: CX3002 is a structurally novel inhibitor of factor Xa, with promising prospects. This study aims to report the results of a first-in-human ascending-dose study of CX3002 in Chinese healthy subjects, and to establish an exploratory population pharmacokinetic/pharmacodynamic (PK/PD) model to investigate the exposure-response relationship of CX3002. Methods: The randomized, double-blind, placebo-controlled study included six single-dose groups and three multiple-dose groups, with a dose range of 1-30 mg. Safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of CX3002 were evaluated. PK of CX3002 was analyzed using both non-compartment method and population modeling. PK/PD model was developed using nonlinear mixed effect modeling approach and was evaluated by prediction-corrected visual predictive check and bootstrap methods. Results: A total of 84 subjects were enrolled and all participants completed the study. CX3002 exhibited satisfactory safety and tolerability in healthy subjects. C max and AUC of CX3002 increased with dose from 1 to 30 mg, but less-than-proportional increases were observed. There was no obvious accumulation with multiple
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- Author
- Wenjun Chen; Zourong Ruan; Honggang Lou; Lu Wang; Rong Shao; Fenghua Li; Bo Jiang
- Publisher
- Elsevier BV
- Published
- 2023
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)