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Oncology · FDA Approved

Relugolix (Orgovyx)

FDA-approved

How to ask your doctor
Written by Peptide Association Editorial TeamLast reviewed Editorial policy

01 · Overview

Relugolix is an orally active non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist (PMID 32469183). Although it is not a peptide, it acts through the same mechanism as peptide GnRH antagonists, blocking pituitary GnRH receptors to suppress gonadotropin and sex steroid production.

It is approved alone for advanced prostate cancer and, in a once-daily combination with estradiol and norethindrone acetate, for heavy menstrual bleeding associated with uterine fibroids and for moderate to severe endometriosis pain. The oral route offers an alternative to depot peptide formulations.

02 · Research summary & key findings

In the phase 3 HERO trial (NEJM 2020), 96.7% of men on relugolix maintained castration through 48 weeks versus 88.8% on leuprolide, and major adverse cardiovascular events occurred in 2.9% versus 6.2% (PMID 32469183). Relugolix was FDA approved for prostate cancer in 2020 as the first oral GnRH antagonist for this use (PMID 39611541). In the LIBERTY 1 and 2 trials, 73% and 71% of women on relugolix combination therapy met the bleeding endpoint versus 19% and 15% on placebo, with bone density similar to placebo (PMID 33596357); the combination is approved in the US for fibroid-associated heavy menstrual bleeding (PMID 36331779). In HERO, mean testosterone 90 days after stopping treatment was 288.4 ng/dL with relugolix versus 58.6 ng/dL with leuprolide, indicating faster recovery (PMID 32469183).

03 · Regulatory status

Relugolix (Orgovyx) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Relugolix (Orgovyx) is an FDA-approved medicine prescribed for the conditions on its label. It is not part of our intake, so we do not propose protocols for it. If you think it may be relevant to you, talk to your own doctor. How to ask your doctor.

04 · Administration routes

  • Oral

References

  1. [1]Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer N Engl J Med, 2020. PMID 32469183
  2. [2]Treatment of Uterine Fibroid Symptoms with Relugolix Combination Therapy N Engl J Med, 2021. PMID 33596357
  3. [3]Relugolix/Estradiol/Norethisterone (Norethindrone) Acetate: A Review in Symptomatic Uterine Fibroids Drugs, 2022. PMID 36331779
  4. [4]Relugolix for the treatment of prostate cancer Expert Opin Pharmacother, 2024. PMID 39611541

Primary literature

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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol. See our editorial policy for how this content is produced and reviewed. Clinicians: join the network.