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Relugolix FDA Approval Status

FDA Approved: No
Generic name: relugolix
Company: Myovant Sciences
Treatment for: Prostate Cancer, Uterine Fibroids, Endometriosis

Relugolix is an oral gonadotropin-releasing hormone (GnRH) receptor antagonist FDA approved as monotherapy under the brand name Orgovyx for the treatment of men with advanced prostate cancer, and in development for use in combination with estradiol and norethindrone acetate for the treatment of women with heavy menstrual bleeding associated with uterine fibroids and pain associated with endometriosis.

  • Relugolix works by binding to and blocking the GnRH receptor in the anterior pituitary gland. Blocking GnRH receptors decreases the release of gonadotropins (luteinizing hormone and follicle-stimulating hormone) thereby decreasing the production of estrogen and progesterone by the ovaries in women, and testosterone by the testes in men.
  • Monotherapy for Prostate Cancer
    Testosterone contributes to the growth of prostate cancer, and androgen deprivation therapy with GnRH receptor antagonists are used to decrease testosterone levels. Relugolix 120 mg (following a single 360 mg loading dose) is being studied as a monotherapy to decrease testosterone levels in men advanced with prostate cancer.
    Update: FDA Approves Orgovyx (relugolix) as the First Oral Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonist for Advanced Prostate Cancer December 18, 2020
  • Combination Therapy for Uterine Fibroids and Endometriosis
    Estradiol contributes to the growth of uterine fibroids and the pain of endometriosis, and GnRH receptor antagonists reduce ovarian estradiol production. Relugolix 40 mg in combination with estradiol 1.0 mg and norethindrone acetate 0.5 mg is being studied as a combination therapy for the treatment of women with heavy menstrual bleeding associated with uterine fibroids, and pain associated with endometriosis. Low-estrogen levels can weaken bones, and can cause cause unwanted side effects such as hot flashes. Adding low doses of estradiol and progestin in combination with relugolix can offset these effects.

Development Timeline for relugolix

DateArticle
Oct 21, 2020Myovant Sciences Presents Additional Data on Relugolix Combination Therapy from Studies in Endometriosis and Uterine Fibroids
Aug 17, 2020Myovant Sciences Announces FDA Acceptance of New Drug Application for Once-Daily Relugolix Combination Tablet for Uterine Fibroids
Jul  6, 2020Myovant Sciences Presents Additional Data on Relugolix Combination Therapy from Phase 3 LIBERTY Studies in Women with Uterine Fibroids and from Ovulation Inhibition Study
Jun 23, 2020Myovant Sciences Announces Positive Results from Second Phase 3 Study Evaluating Once-Daily Relugolix Combination Therapy in Women with Endometriosis
Jun  1, 2020Sumitovant Biopharma Announces Myovant Sciences’ Submission of New Drug Application (NDA) to the FDA for Once-Daily Relugolix Combination Tablet for the Treatment of Women with Uterine Fibroids
Jun  1, 2020Myovant Sciences Submits New Drug Application (NDA) to the FDA for Once-Daily Relugolix Combination Tablet for the Treatment of Women with Uterine Fibroids
May 14, 2019Myovant Sciences Announces Positive Phase 3 Results from LIBERTY 1 Study Evaluating Once Daily Relugolix Combination Therapy in Women with Uterine Fibroids

Further information

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