Study of Relugolix Alone and Relugolix Combined With Hormonal Add-Back Therapy in Healthy Premenopausal Female Participants

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: Relugolix; Drug: E2/NETA

• Registration Number: NCT04978688
• Lead Sponsor: Myovant Sciences GmbH

Brief Summary

This was a randomized, open-label, repeat dose study of once daily relugolix alone or relugolix combined with hormonal add-back therapy (combination estradiol/norethindrone acetate) (E2/NETA) to assess safety, including markers of bone resorption, pharmacokinetics (PK), and pharmacodynamics (PD) endpoints.

Detailed Description

Not available

Study Timeline

• Study Start: 2016-06-16
• Primary Completion: 2016-09-21
• Study Completion: 2016-09-21
• Status Verified: 2021-07
• Study First Submitted: 2021-07-20
• Study First Submitted QC: 2021-07-20
• Last Update Submitted: 2021-07-20
• Study First Posted: 2021-07-27
• Last Update Posted: 2021-07-27

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Female
• Target Recruitment: 48

Inclusion Criteria

1. Pre-menopausal female between 18 and 48 years of age.
2. E2, P, LH and FSH concentrations within 0.5x of the lower limits of normal range and 2x of the upper limits of normal upper limits of normal range (ULN)
3. Regular menstrual periods for the 3 months prior to study enrollment
4. Body weight ≥ 45 killograms (kgs) and body mass index (BMI) of 20 to 36
5. Capable of giving written informed consent

Exclusion Criteria

1. Pregnancy
2. Lactating Females
3. Any contraindication to the treatment with E2 and NETA
4. Use of the following medications in the 3 months prior to screening: injectable hormonal contraceptives, sex hormone medications or danazol
5. Use of the following medications in the 6 months prior to screening: injectable gonadotropin-releasing hormone agonists, hormonal, or non-hormonal intrauterine devices
6. History of sensitivity to any of the study medications of components thereof or history of drug
7. Significant gynecological, endocrine, metabolic or other health conditions
8. History of regular alcohol consumption within 6 months of study

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Relugolix + E2/NETA	Relugolix	Participants received relugolix 40 mg and E2/NETA at 1 mg/ 0.5 mg for 6 weeks.
Relugolix + E2/NETA	E2/NETA	Participants received relugolix 40 mg and E2/NETA at 1 mg/ 0.5 mg for 6 weeks.
Relugolix	Relugolix	Participants received relugolix 40 milligrams (mg) alone for 6 weeks.

Primary Outcome Measures

Name	Time	Method
PK: Area Under The Concentration-Time Curve From Time Zero To Hour 24 (AUC0-24) Of Relugolix, E2, Estrone (El), Ethinylestradiol (EE), NETA	Predose and up to 24 hours at Weeks 3 and 6
PK: Maximum Concentration (Cmax) Of Relugolix, E2, El, NETA	Predose and up to 24 hours at Weeks 3 and 6
PK: Time To Maximum Concentration (Tmax) Of Relugolix, E2, El, EE, NETA	Predose and up to 24 hours at Weeks 3 and 6

Secondary Outcome Measures

Name	Time	Method
Change From Baseline In Serum Follicle Stimulating Hormone (FSH) At Week 6	Baseline, Week 6
Incidence Of Treatment-Emergent Adverse Events	8 weeks
Change From Baseline In Serum Luteinizing Hormone (LH) At Week 6	Baseline, Week 6
Incidence Of Hot Flush	8 weeks
Change From Baseline In Serum Progesterone (P) At Week 6	Baseline, Week 6
Change From Baseline In Serum E2 And E1 At Week 6	Baseline, Week 6
Change From Baseline In N-telopeptide And C-telopepetide Concentrations At Week 6	Baseline, Week 6

Trial Locations

Locations (1)

Clinical Study Site; 🇺🇸 Minneapolis, Minnesota, United States