NCT04714554

A Study of the Effects of Erythromycin on the Pharmacokinetics of Relugolix, Estradiol, and Norethindrone in Healthy Postmenopausal Women and on the Pharmacokinetics of Relugolix in Healthy Adult Men

A Two-Part, Open-Label, Fixed-Sequence, Two-Period Crossover Study to Assess the Effects of Erythromycin on the Pharmacokinetics of Relugolix, Estradiol, and Norethindrone After Administration of the Relugolix/Estradiol/Norethindrone Acetate Fixed-Dose Combination Tablet in Healthy Postmenopausal Women and on the Pharmacokinetics of Relugolix After Administration of a Single 120-mg Dose in Healthy Adult Men

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 43 (actual)
• Sponsor: Myovant Sciences GmbH · Industry
• Sex: All
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

This is a two-part, open-label, fixed-sequence, two-period crossover drug interaction study to assess the potential effects of erythromycin on the pharmacokinetics of relugolix, estradiol (E2), and norethindrone (NET) in healthy postmenopausal women (Part 1) and the pharmacokinetics of relugolix in healthy adult men (Part 2).

Detailed description

Each study part consists of two sequential treatment periods (Treatment Period 1 and Treatment Period 2) in which study participants will receive study treatments in a fixed (single)-sequence, crossover manner. In Part 1 of the study, a single relugolix/E2/norethindrone acetate (NETA) (40 milligrams \[mg\]/1 mg/0.5 mg) fixed-dose combination (FDC) tablet will be administered alone on Day 1 of Treatment Period 1; in Treatment Period 2, erythromycin will be administered on Day 1 to Day 12 (500 mg, four times daily \[QID\]) with co-administration of a single FDC tablet with the morning dose of erythromycin on Day 8. In Part 2 of the study, a single 120-mg dose of relugolix will be administered alone on Day 1 of Treatment Period 1; in Treatment Period 2, erythromycin will be administered on Day 1 to Day 12 (500 mg QID) with co-administration of a single 120-mg dose of relugolix with the morning dose of erythromycin on Day 8. There will be a nine-day washout interval between administration of study drug (the FDC tablet \[Part 1\] or relugolix 120 mg \[Part 2\]) on Day 1 of Treatment Period 1 and Treatment Period 2.

Conditions

• Healthy

Interventions

Type	Name	Description
DRUG	Relugolix/E2/NETA FDC	Relugolix/E2/NETA (40 mg/1 mg/0.5 mg) FDC tablet; oral administration.
DRUG	Relugolix	Relugolix 120-mg tablets; oral administration.
DRUG	Erythromycin	Erythromycin 500-mg tablets; oral administration.

Timeline

• Start date: 2021-01-06
• Primary completion: 2021-03-29
• Completion: 2021-03-29
• First posted: 2021-01-19
• Last updated: 2021-09-01

Locations

1 site across 1 country: United States

Regulatory

• FDA-regulated drug study