Orgovyx, Myfembree
Evidence Grade A — Regulatory approved. 234 published studies. 42 registered clinical trials.
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Relugolix is a daily oral tablet that suppresses sex hormone production — the first oral option for advanced prostate cancer (as Orgovyx) and a component of combination therapy for uterine fibroids and endometriosis (as Myfembree). Like elagolix, it is not a peptide but a small molecule that targets the same GnRH pathway as injectable peptide treatments. It eliminates the need for clinic visits for injections.
234 published studies: 160 human, 1 animal, 6 in-vitro, 70 reviews
Relugolix is marketed as Orgovyx for advanced prostate cancer (approved December 2020) and as a component of Myfembree for uterine fibroids (approved May 2021) and endometriosis pain (approved August 2022). The landmark HERO trial compared relugolix directly against leuprolide in over 900 prostate cancer patients.
HERO showed relugolix achieved sustained testosterone suppression in 96.7% of patients versus 88.8% with leuprolide injections — and crucially, the rate of major cardiovascular events was halved (2.9% versus 6.2%). This cardiovascular advantage has been a significant factor in its adoption, particularly for patients with existing heart disease. As a daily oral tablet, it eliminates the need for clinic visits for injections. Like elagolix, relugolix is not a peptide but targets the same GnRH pathway and is included in this database for that reason.
Relugolix directly blocks the GnRH receptor in the pituitary gland, rapidly shutting down testosterone or oestrogen production without the initial hormone surge seen with traditional GnRH agonist injections. As an oral tablet, it offers a completely non-invasive alternative to injections or implants. Hormone suppression begins rapidly, with over half of prostate cancer patients reaching castrate testosterone levels within four days of starting treatment. Effects reverse quickly after stopping — testosterone typically recovers within 90 days.
The HERO trial compared relugolix directly against injectable leuprolide in over 900 prostate cancer patients. Relugolix achieved superior testosterone suppression (96.7% vs 88.8%) and — crucially — halved the rate of major cardiovascular events (2.9% vs 6.2%). This heart safety advantage is clinically meaningful because hormone suppression therapy for prostate cancer is known to increase cardiovascular risk. As a daily tablet, relugolix offers significant convenience over monthly or quarterly injections and avoids the initial hormone surge ("flare") that occurs with older GnRH agonist treatments. Testosterone recovery after stopping is rapid (median 90 days), which is relevant for patients using intermittent therapy strategies. The Myfembree combination product for fibroids and endometriosis includes built-in hormone add-back therapy to mitigate bone density loss.
Relugolix for Endometriosis Associated Pain
Estradiol-mediated Inflammation and Central Sensitization in the Pathophysiology of Endometriosis-associated Pelvic Pain
REDI-CaP(Recovery of Erectile Dysfunction Induced in Prostate Cancer Patients)
Optimal PSA Triggered Individual Management of Androgen Sensitive Prostate Cancer
Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA Trial
FDA ORIG 1
FDA ORIG 1
EMA Marketing Authorisation
FDA SUPPL 2
FDA SUPPL 5
FDA SUPPL 6
FDA SUPPL 4
Health Canada Market Authorisation
FDA SUPPL 7
FDA SUPPL 8
FDA SUPPL 6
FDA SUPPL 12
FDA SUPPL 12
Histrelin is available as Supprelin LA for central precocious puberty (approved 2007). The Vantas implant for prostate cancer was approved in 2004 but discontinued in 2021. The implant requires a minor surgical procedure for insertion and removal/replacement each year. Supprelin LA's main clinical advantage is its 12-month duration — the longest of any GnRH agonist — which is particularly valuable in paediatric patients where treatment compliance over years is important. Clinical studies demonstrated effective suppression of puberty markers in over 97% of patients. The implant has also seen significant off-label use in gender-affirming care as a puberty blocker, where its annual dosing schedule offers practical benefits for adolescent patients and their families.
Goserelin is marketed as Zoladex by AstraZeneca, available as 3.6 mg monthly and 10.8 mg three-monthly subcutaneous implants. First approved in 1989, it is used in advanced prostate cancer, premenopausal breast cancer, endometriosis, and for thinning the uterine lining before surgical procedures. Goserelin achieves castrate-level testosterone suppression (below 50 ng/dL) within two to four weeks. Its unique implant delivery system means there is no liquid injection, reconstitution, or refrigeration required — a practical advantage in some clinical settings. Like all GnRH agonists, it causes an initial hormone flare before suppression takes effect. Goserelin holds an important niche in breast cancer treatment, where it is used to suppress ovarian function in premenopausal women with hormone-receptor-positive disease, often in combination with aromatase inhibitors.
Nafarelin is marketed as Synarel (approved 1990) for endometriosis and central precocious puberty. It requires administration as one spray in each nostril twice daily — a higher frequency than injectable alternatives but avoids needles entirely, which can be a significant advantage for some patients, particularly children. Clinical trials showed symptom improvement in 75–92% of endometriosis patients. However, absorption can be affected by nasal congestion or concurrent use of nasal decongestants, which can be a practical limitation. As with all GnRH agonists, prolonged use leads to bone density loss, and treatment for endometriosis is typically limited to six months. Nafarelin occupies a niche for patients who prefer non-injectable hormone suppression, though it has become less commonly prescribed as longer-acting depot injections and oral alternatives have become available.
