Relugolix Combination Tablets in Healthy Japanese Premenopausal Women: Pharmacokinetics, Pharmacodynamics, and Safety Profile.

ABSTRACT:

Purpose

To evaluate the applicability of overseas-approved dosage of relugolix combination tablets (relugolix 40 mg, estradiol [E2] 1 mg, and norethisterone acetate 0.5 mg) in healthy premenopausal Japanese women.

Methods

A randomized, double-blind phase I/II study was conducted to compare the pharmacokinetics, pharmacodynamics, and safety of repeated once-daily administration of relugolix combination tablets and relugolix (40 mg) for 6 weeks.

Results

There were 26 participants in each treatment group. The mean maximum concentration and area under the concentration-time curve from time zero to 24 h ratios for relugolix (relugolix combination tablet group/relugolix group) were both approximately 0.7-0.9. The mean E2 level ranged from 20 to 50 pg/mL. There was no notabl

SUBMITTER: Osuga Y 

PROVIDER: S-EPMC12657618 | biostudies-literature | 2025 Jan-Dec

REPOSITORIES: biostudies-literature