Relugolix FDA Approval Status
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
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