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FDA Approved Sexual & Reproductive Health

Relugolix

also known as: Orgovyx, Relumina, TAK-385

The oral alternative to Lupron — a once-daily pill that suppresses testosterone to castrate levels for prostate cancer without the flare, injection, or cold-chain requirements of injectable GnRH agonists.

A non-peptide oral GnRH receptor antagonist achieving castrate testosterone levels within days (vs. weeks for leuprolide), FDA-approved for advanced prostate cancer and uterine fibroids.

Mechanism of action

Competitive antagonist at the pituitary GnRH receptor. Rapidly suppresses LH and FSH without the initial agonist flare seen with GnRH agonists. In prostate cancer, this achieves medical castration. Unlike depot GnRH agonists, testosterone recovery occurs within weeks of discontinuation.

Primary uses

  • Advanced prostate cancer (androgen deprivation therapy)
  • Uterine fibroids (as Myfembree combination)
  • Endometriosis (Japan)

Typical dosing

120 mg once daily (after 360 mg loading dose on Day 1) (oral)

Loading dose of 360 mg on Day 1 accelerates testosterone suppression. Take without food or with a low-fat meal.

Regulatory status

FDA-approved in 2020 (Orgovyx, Myovant Sciences) for advanced prostate cancer. Also approved in combination with estradiol/norethindrone (Myfembree) for uterine fibroids (2021). Approved in Japan as Relumina for uterine fibroids.

References

  1. [clinical-trial] Shore ND, et al. "Oral relugolix for androgen-deprivation therapy in advanced prostate cancer (HERO)." N Engl J Med, 2020;382:2187-2196.
  2. [fda-pi] Orgovyx (relugolix) Prescribing Information. Myovant Sciences.

Related peptides

Leuprolide

The prototypical long-acting GnRH agonist, FDA-approved across multiple formulations (Lupron Depot, Eligard, Fensolvi, Camcevi) for advanced prostate cancer, endometriosis, central precocious puberty, uterine fibroids, and IVF protocols.

Elagolix

The first oral GnRH antagonist — a non-peptide small molecule that suppresses estrogen production without injection, FDA-approved for endometriosis pain.

Degarelix

Ferring's Firmagon — a GnRH antagonist for advanced prostate cancer that achieves castrate testosterone within 3 days, eliminating the clinical flare risk of GnRH-agonist therapy in patients with symptomatic bone metastases or impending spinal cord compression.

Goserelin

AstraZeneca's Zoladex — a long-acting GnRH agonist delivered as a subcutaneous biodegradable implant. FDA-approved for advanced prostate cancer, advanced breast cancer in premenopausal women, endometriosis, and endometrial thinning prior to ablation.
Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.