Study of Relugolix in Men With Metastatic Castration-Sensitive Prostate Cancer or Non-Metastatic or Metastatic Castration-Resistant Prostate Cancer

NCT04666129 | Completed Phase 1 FDA Drug

• 1 other identifier: MVT-601-049
• Study Type: interventional
• Target: 48
• Locations: 1 country
• Sites: 16

Brief Summary

This study is being conducted to assess the safety and tolerability of relugolix with other agents approved for use in combination with androgen deprivation therapy (ADT) for a 12-week treatment period and an additional 40-week safety extension period in men with prostate cancer, either metastatic castration-sensitive prostate cancer (mCSPC) or non-metastatic or metastatic castration-resistant prostate cancer (nmCRPC or mCRPC).

Conditions

Metastatic Castration-Resistant Prostate Cancer; Metastatic Castration-Sensitive Prostate Cancer; Non-Metastatic Castration-Resistant Prostate Cancer

Keywords

mCRPC; mCSPC; Relugolix; Abiraterone; Prednisone; Leuprolide acetate; nmCRPC; Apalutamide; Docetaxel; Degarelix; Methylprednisolone

Outcome Measures

Primary Outcomes (1)

• Incidence of Adverse Events

  Parts 1, 2, and 3

  Baseline through Week 13

Secondary Outcomes (9)

• Mean Testosterone Serum Concentrations at Baseline (Day 1), Week 5, and Week 13

  Baseline (Day 1), Week 5, and Week 13

• Number and Proportion of Participants with Testosterone Concentrations ≥ 50 ng/dL at Baseline (Day 1), Week 5, and Week 13

  Baseline (Day 1), Week 5, and Week 13

• Relugolix Trough Concentrations at Baseline (Day 1), Week 3, Week 5, Week 9, and Week 13

  Baseline (Day 1), Week 3, Week 5, Week 9, and Week 13

• Apalutamide and N-desmethyl Apalutamide Trough Concentrations at Baseline (Day 1), Week 3, Week 5, Week 9, and Week 13

  Baseline (Day 1), Week 3, Week 5, Week 9, and Week 13

• Mean Testosterone Serum Concentrations at Baseline (Day 1), Mid-Treatment, and Week 13

  Baseline (Day 1), Mid-Treatment, and Week 13

Study Arms (3)

Part 1: Relugolix plus Abiraterone plus a Corticosteroid

EXPERIMENTAL

Participants will receive relugolix in combination with abiraterone plus a corticosteroid for 12 weeks during the study treatment period.

Drug: Relugolix; Drug: Abiraterone; Drug: Prednisone; Drug: Methylprednisolone

Part 2: Relugolix plus Apalutamide

EXPERIMENTAL

Participants will receive relugolix in combination with apalutamide for 12 weeks during the study treatment period.

Drug: Relugolix; Drug: Apalutamide

Part 3: Relugolix plus Docetaxel with or without Prednisone

EXPERIMENTAL

Participants will receive relugolix in combination with docetaxel with or without prednisone for 12 weeks during the study treatment period.

Drug: Relugolix; Drug: Prednisone; Drug: Docetaxel

Interventions

Relugolix DRUG

(Part 1 and Part 3) Relugolix will be administered orally as a single 360-milligram (mg) loading dose of 3 x 120-mg tablets, followed by a 120-mg dose (1 x 120-mg tablets), taken once daily at approximately the same time each day. (Part 2) Relugolix will be administered orally as a single 360-milligram (mg) loading dose of 3 x 120-mg tablets, followed by a 240-mg dose (2 x 120-mg tablets), taken once daily at approximately the same time each day.

Also known as: MVT-601, TAK-385, T-1331285, RVT-601, Orgovyx

Part 1: Relugolix plus Abiraterone plus a Corticosteroid; Part 2: Relugolix plus Apalutamide; Part 3: Relugolix plus Docetaxel with or without Prednisone

Abiraterone DRUG

Abiraterone acetate (1000 mg \[2 x 500-mg tablets\]) or fine-particle abiraterone acetate (500 mg \[4 x 125-mg tablets\]) will be administered orally once daily.

Also known as: Zytiga, Yonsa

Part 1: Relugolix plus Abiraterone plus a Corticosteroid

Prednisone DRUG

(Part 1 only) For participants with mCSPC, a 5-mg dose of prednisone will be administered orally once daily, and for participants with mCRPC, a 5-mg dose of prednisone will be administered orally twice daily. (Part 3 only) Prednisone 5 mg can be administered orally twice daily but is not required.

Part 1: Relugolix plus Abiraterone plus a Corticosteroid; Part 3: Relugolix plus Docetaxel with or without Prednisone

Methylprednisolone DRUG

For participants with mCRPC taking fine-particle abiraterone acetate, methylprednisolone 4 mg will be administered orally twice daily.

Also known as: Medrol

Part 1: Relugolix plus Abiraterone plus a Corticosteroid

Apalutamide DRUG

Apalutamide 240 mg (4 x 60-mg tablets) will be administered orally once daily.

Also known as: Erleada

Part 2: Relugolix plus Apalutamide

Docetaxel DRUG

Docetaxel 75 mg/m2 dose will be administered every 3 weeks as a 1-hour intravenous infusion.

Also known as: Docefrez, Taxotere

Part 3: Relugolix plus Docetaxel with or without Prednisone

Eligibility Criteria

• Age: 18 Years+
• Sex: male
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• A previous diagnosis of adenocarcinoma of the prostate confirmed by histologic or cytologic evidence and with a documented medical history of either:
• mCSPC (Parts 1, 2, and 3) defined as having at least two of three risk factors at the baseline (Day 1) visit:
• Total Gleason score of ≥ 6; and
• Presence of ≥ 2 metastatic lesions on bone scan; OR
• Radiologic evidence of measurable visceral metastases with exception of hepatic metastases.
• nmCRPC (Part 2 only) defined as disease progression despite maintaining castration levels of testosterone with androgen deprivation therapy (ADT), as evidenced by an increase in consecutive prostate-specific antigen (PSA) concentrations (2 measurements, at least one week apart).
• mCRPC (Parts 1 and 3) defined as disease progression despite maintaining castration levels of testosterone with ADT:
• An increase in consecutive PSA (2 measurements at least 1 week apart); or
• Worsening clinical symptoms; or
• Radiologic evidence demonstrating enlarged metastatic lesions or the development of new metastases.
• Initiating treatment or currently receiving treatment of leuprolide acetate (3-, 4-, or 6-month injections \[intramuscular Lupron or subcutaneous Eligard\]) or another GnRH receptor agonist (triptorelin) or a GnRH receptor antagonist (degarelix or relugolix \[maximum duration of 3 months\]) in combination with:
• Part 1: abiraterone acetate 1000 mg or fine-particle abiraterone acetate 500 mg once daily plus prednisone 5 mg once daily for participants with mCSPC or twice daily for participants with mCRPC or methylprednisolone 4 mg once daily and in whom abiraterone has been well tolerated (that is, without evidence of hepatotoxicity requiring dose adjustment for abiraterone).
• Part 2: apalutamide 240 mg once daily and in whom apalutamide has been well tolerated (that is, without a fracture, fall, or seizure episode or need to dose adjust due to any adverse events).
• Part 3: docetaxel 75 mg/m2 and in whom docetaxel has been well tolerated (that is, no evidence of hypersensitivity reaction, febrile neutropenia or neutrophils \< 500 cells/mm3 for more than 1 week, severe or cumulative cutaneous reactions, or moderate neurosensory signs and/or symptoms despite dose reduction). Note: Patients receiving treatment with another agent in addition to docetaxel, such as a steroid synthesis inhibitor or androgen receptor antagonist, may be enrolled.

You may not qualify if:

• A medical history of brain or hepatic metastases based on radiologic evidence or a medical history of surgical castration;
• Received combination treatment with a GnRH analog or GnRH receptor antagonist with either abiraterone acetate plus a corticosteroid (Part 1) or apalutamide (Part 2) in patients with mCSPC (Part 1 and Part 2) or nmCRPC (Part 2) for a total duration \> 24 months or in patients with mCRPC (Part 1) for a total duration \> 6 months;
• Is scheduled or anticipates being scheduled for major surgery during the study treatment period;
• A current diagnosis of a malignancy other than prostate cancer, with the exception of any of the following:
• Adequately treated basal cell carcinoma or squamous cell carcinoma of the skin, or carcinoma in situ of any type;
• Adequately treated Stage I cancer that is currently in remission and has been in remission for ≥ 2 years;
• Any other cancer from which the patient has been disease-free for ≥ 3 years;
• Abnormal clinical laboratory test value(s) at the screening visit or prior to the baseline (Day 1) visit including:
• Serum creatinine \> 2.0 mg/dL;
• Platelets \< 100 × 103/μL;
• Hemoglobin \< 10.0 g/dL;
• Leukocytes (WBC) \< 3 × 103/μL;
• Absolute neutrophil count \< 1.5 × 103/μL;
• Hemoglobin A1c (HbA1c) \> 8%; Note (Part 3 only): Transfusions and/or administration of growth factors are permitted as indicated for the clinical management of docetaxel-related hematologic effects and in accordance with the investigator's judgement.
• Known hepatic disease, including alcoholic liver disease or viral hepatitis such as hepatitis A (hepatitis A virus IgM positive), chronic hepatitis B (HbsAg positive), or chronic hepatitis C (HCV antibody positive, confirmed by HCV RNA) or clinical signs of hepatic disease such as jaundice;

Sponsors & Collaborators

• Sumitomo Pharma America, Inc.: lead

Study Sites (16)

Urological Associates of Southern Arizona, P.C.

Tucson, Arizona, 85741, United States

Location

Arkansas Urology

Little Rock, Arkansas, 72211, United States

Location

Colorodo Clinical Research

Lakewood, Colorado, 80228, United States

Location

Chesapeake Urology Research Associates

Baltimore, Maryland, 21204, United States

Location

University of Massachusetts Medical School

Worcester, Massachusetts, 01655, United States

Location

New Jersey Urology

Saddle Brook, New Jersey, 07663, United States

Location

Clinical Research Alliance, Inc.

Westbury, New York, 11590, United States

Location

Alliance Urology

Greensboro, North Carolina, 27403, United States

Location

Wake Forest Baptist Health

Winston-Salem, North Carolina, 27157, United States

Location

Helios Clinical Research, LLC.

Middleburg Heights, Ohio, 44130, United States

Location

Center for Advanced Urology, LLP d/b/a: MidLantic Urology

Bala-Cynwyd, Pennsylvania, 19004, United States

Location

Keystone Urology Specialists

Lancaster, Pennsylvania, 17604, United States

Location

Carolina Urologic Research Center

Myrtle Beach, South Carolina, 29572, United States

Location

Urology Associates, P.C.

Nashville, Tennessee, 37209, United States

Location

UT Southwestern Medical Center

Dallas, Texas, 75390, United States

Location

Urology San Antonio

San Antonio, Texas, 78229, United States

Location

Related Publications (2)

• De La Cerda J, Belkoff L, Courtney KD, Diamond E, D'Olimpio J, Dunshee C, Gervasi L, Goodman M, Mittal K, Morris D, Sieber P, Tutrone R, Ryan M, Zhong Y, Ufer M, Shore N. Safety and Tolerability of Relugolix in Combination with Abiraterone or Apalutamide for Treatment of Patients with Advanced Prostate Cancer: Data from a 52-Week Clinical Trial. Target Oncol. 2025 May;20(3):503-517. doi: 10.1007/s11523-025-01139-3. Epub 2025 Apr 4.

  PMID: 40180682 DERIVED

• De La Cerda J, Dunshee C, Gervasi L, Sieber P, Belkoff L, Tutrone R, Lu S, Gatoulis SC, Brown B, Migoya E, Shore N. A Phase I Clinical Trial Evaluating the Safety and Dosing of Relugolix with Novel Hormonal Therapy for the Treatment of Advanced Prostate Cancer. Target Oncol. 2023 May;18(3):383-390. doi: 10.1007/s11523-023-00967-5. Epub 2023 Apr 15.

  PMID: 37060432 DERIVED

MeSH Terms

Interventions

relugolix; abiraterone; Abiraterone Acetate; Prednisone; Methylprednisolone; apalutamide; Docetaxel

Intervention Hierarchy (Ancestors)

Androstenes; Androstanes; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Pregnadienediols; Pregnadienes; Pregnanes; Prednisolone; Pregnadienetriols; Taxoids; Cyclodecanes; Cycloparaffins; Hydrocarbons, Alicyclic; Hydrocarbons, Cyclic; Hydrocarbons; Organic Chemicals; Diterpenes; Terpenes

Study Officials

• Mike Ufer

  Sumitomo Pharma America, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 7, 2020
• First Posted: December 14, 2020
• Study Start: February 18, 2021
• Primary Completion: May 28, 2024
• Study Completion: May 28, 2024
• Last Updated: August 17, 2025

Record last verified: 2025-08

Data Sharing

• IPD Sharing: Will not share

Locations

US (16)