Relugolix
Relugolix is a GnRH receptor antagonist used primarily for treating advanced prostate cancer and heavy menstrual bleeding associated with uterine fibroids. It works by blocking GnRH receptors in the pituitary gland, which reduces the release of LH and FSH hormones, leading to decreased testosterone production.
Relugolix is an oral GnRH antagonist that lowers testosterone levels to treat prostate cancer and uterine fibroids.
Key facts at a glance
- ATC
- L02BX04
- RxNorm
- 2472778
- Generic
- Relugolix
- Class
- atc-l02
- Brands
- Orgovyx, Myfembree
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Advanced prostate cancer and moderate-to-severe symptoms of uterine fibroids (leiomyomas) in premenopausal women, such as heavy menstrual bleeding.
Relugolix competitively binds to pituitary GnRH receptors, blocking the action of natural GnRH. This suppresses the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn reduces testicular testosterone production.
Common side effects include hot flashes, fatigue, and musculoskeletal pain. It may cause fetal harm if used during pregnancy. Regular monitoring of testosterone levels and liver function may be recommended. Unlike injectable GnRH agonists, oral relugolix does not cause an initial testosterone surge.
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy