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).
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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
43
Relugolix/E2/NETA (40 mg/1 mg/0.5 mg) FDC tablet; oral administration.
Relugolix 120-mg tablets; oral administration.
Erythromycin 500-mg tablets; oral administration.
Clinical Pharmacology of Miami, An Evolution Research Group Portfolio Company
Hialeah, Florida, United States
Area Under The Concentration-time Curve From Time 0 Extrapolated To Infinity (AUC0-inf) Of Relugolix Or Other Analytes
Time frame: Day 8 predose and up to 120 hours postdose at multiple time points during Treatment Period 2 (Study Days 10 to 22)
Maximum Plasma Concentration (Cmax) Of Relugolix Or Other Analytes
Time frame: Day 8 predose and up to 120 hours postdose at multiple time points during Treatment Period 2 (Study Days 10 to 22)
Overall Incidence Of Adverse Events
Time frame: 10 Weeks
Predose Trough Plasma Concentrations (Ctrough) Of Erythromycin
Time frame: Predose on Day 7 and 8 of Treatment Period 2 (Study Days 10 to 22)
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