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

A Randomized Open Label Study to Evaluate the Safety, PK, and PD of Relugolix Alone and Relugolix Combined With Hormonal Add-Back Therapy for 6 Weeks in Healthy Premenopausal Female Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Relugolix; Drug: E2/NETA

• Study Type: Interventional
• Enrollment (Actual): 48
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Minnesota
    • Minneapolis, Minnesota, United States, 55404
      • Clinical Study Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 48 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Female

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Relugolix; Participants received relugolix 40 milligrams (mg) alone for 6 weeks.	Drug: Relugolix; Administered as an oral tablet once daily.
Experimental: Relugolix + E2/NETA; Participants received relugolix 40 mg and E2/NETA at 1 mg/ 0.5 mg for 6 weeks.	Drug: Relugolix; Administered as an oral tablet once daily.; Drug: E2/NETA; Administered as an oral tablet once daily.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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

Outcome Measure	Time Frame
Change From Baseline In Serum Follicle Stimulating Hormone (FSH) At Week 6	Baseline, Week 6
Change From Baseline In Serum Luteinizing Hormone (LH) At Week 6	Baseline, Week 6
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
Incidence Of Treatment-Emergent Adverse Events	8 weeks
Incidence Of Hot Flush	8 weeks

Collaborators and Investigators

• Sponsor: Myovant Sciences GmbH

Study record dates

Study Major Dates

• Study Start (Actual): June 16, 2016
• Primary Completion (Actual): September 21, 2016
• Study Completion (Actual): September 21, 2016

Study Registration Dates

• First Submitted: July 20, 2021
• First Submitted That Met QC Criteria: July 20, 2021
• First Posted (Actual): July 27, 2021

Study Record Updates

• Last Update Posted (Actual): July 27, 2021
• Last Update Submitted That Met QC Criteria: July 20, 2021
• Last Verified: July 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Hormones, Hormone Substitutes, and Hormone Antagonists; Hormone Antagonists; Androgen Antagonists; Relugolix
• Other Study ID Numbers: MVT-601-1001

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No