Population Pharmacokinetics Modeling and Simulation of Deutenzalutamide, A Novel Androgen Receptor Antagonist, in Patients With Metastatic Castration-Resistant Prostate Cancer

Clin Pharmacol Drug Dev. 2024 Dec;13(12):1291-1300. doi: 10.1002/cpdd.1477. Epub 2024 Oct 4.

Abstract

Deutenzalutamide is a new molecular entity androgen receptor antagonist. The primary aim of this study was to develop a population pharmacokinetic model of deutenzalutamide and evaluate effects of intrinsic and extrinsic factors on pharmacokinetics. A nonlinear mixed-effects modeling approach was performed to develop the population pharmacokinetic of deutenzalutamide using data from 1 Phase I trial of deutenzalutamide. Goodness-of-fit plots, prediction-corrected visual predictive check, and bootstrap analysis were carried out to evaluate the final model. Simulation for the developed model was used to evaluate the covariate effects on the pharmacokinetics of deutenzalutamide. A 2-compartment model with first-order absorption and elimination from the central compartment was established for deutenzalutamide. The final covariate included body weight on peripheral compartment volume. This is the first research developing the population pharmacokinetic model of deutenzalutamide in patients with metastatic castration-resistant prostate cancer, and it is expected to support the future clinical administration of deutenzalutamide.

Keywords: HC‐1119; androgen receptor antagonist; deutenzalutamide; modeling and simulation; population pharmacokinetics.

Publication types

  • Clinical Trial, Phase I

MeSH terms

  • Aged
  • Androgen Receptor Antagonists* / administration & dosage
  • Androgen Receptor Antagonists* / pharmacokinetics
  • Computer Simulation*
  • Humans
  • Male
  • Middle Aged
  • Models, Biological*
  • Neoplasm Metastasis
  • Nonlinear Dynamics
  • Prostatic Neoplasms, Castration-Resistant* / drug therapy

Substances

  • Androgen Receptor Antagonists