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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04978688

Enrollment

Registered

2021-07-27

Start date

2016-06-16

Completion date

2016-09-21

Last updated

2021-07-27

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

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.

Interventions

DRUGRelugolix

Administered as an oral tablet once daily.

DRUGE2/NETA

Administered as an oral tablet once daily.

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

FEMALE

Age

18 Years to 48 Years

Healthy volunteers

Yes

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

Design outcomes

Primary

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

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

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 9, 2026