Clinical Pharmacokinetics of the Androgen Receptor Inhibitor Darolutamide in Healthy Subjects and Patients with Hepatic or Renal Impairment.

ABSTRACT:

Background

Darolutamide is a second-generation androgen receptor inhibitor approved for the treatment of nonmetastatic castration-resistant prostate cancer at a dosage of 600 mg orally twice daily.

Objective

We aimed to fully characterize the pharmacokinetic profile of darolutamide, its diastereomers, and its main active metabolite, keto-darolutamide.

Methods

Single-dose and multiple-dose pharmacokinetics of ¹⁴C-labeled and non-labeled darolutamide were evaluated in healthy subjects and patients with hepatic or renal impairment.

Results

Following darolutamide oral tablet administration, peak plasma concentrations were reached 4-6 h after dosing. Darolutamide elimination was characterized by a half-life of 13 h. Steady state was reached after approxim

SUBMITTER: Zurth C 

PROVIDER: S-EPMC8975796 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature