Evidence Grade A — Regulatory approved. 248 published studies. 57 registered clinical trials.
Medically reviewed by a licensed medical professional
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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.
Relugolix is also known by these brand and alternate names:
248 published studies: 168 human, 1 animal, 6 in-vitro, 73 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.
PeptideTrace tracks 57 registered clinical trials for Relugolix sourced from ClinicalTrials.gov.
Relugolix for Endometriosis Associated Pain
Insights in Endocervical Mucus Secretion
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
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
Relugolix is an oral, non-peptide small molecule GnRH receptor antagonist with an IC₅₀ of 0.12 nM. It is NOT a peptide. It was the first oral GnRH antagonist for prostate cancer and is also used in fixed-dose combination for uterine fibroids and endometriosis.
Relugolix competitively antagonizes the GnRH receptor, directly blocking GnRH-stimulated LH and FSH release. As an antagonist, it provides rapid onset of testosterone suppression without flare—within 4 days, 56% of patients achieved castrate testosterone versus 0% with leuprolide. Its oral bioavailability and potency enable effective HPG axis suppression with a single daily tablet.
Relugolix is marketed as Orgovyx (advanced prostate cancer, approved December 18, 2020) and as a component of Myfembree (relugolix 40 mg + estradiol 1 mg + norethindrone acetate 0.5 mg, for uterine fibroids approved May 26, 2021, and endometriosis-associated pain approved August 5, 2022). In the HERO trial (N=934), relugolix achieved sustained castration in 96.7% versus 88.8% for leuprolide (P<0.001 for superiority). MACE occurred in 2.9% versus 6.2% (54% reduction).
Carbetocin has not been approved by the FDA. It is registered in over 80 countries for prevention of uterine atony and excessive bleeding after caesarean delivery. A heat-stable formulation was added to the WHO Essential Medicines List in 2019. The CHAMPION trial (WHO, 2018; over 29,000 women) compared a heat-stable carbetocin formulation to oxytocin for preventing postpartum haemorrhage after vaginal delivery, and found it to be non-inferior. The heat-stable formulation addresses a significant limitation of oxytocin, which degrades in warm climates without refrigeration — a major concern in low-resource settings where postpartum haemorrhage causes the most deaths. Its regulatory status varies by jurisdiction.
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.
Triptorelin is marketed as Trelstar (approved 2000) for advanced prostate cancer, available as intramuscular depot injections in monthly (3.75 mg), three-monthly (11.25 mg), and six-monthly (22.5 mg) formulations. It is also widely used internationally for gender-affirming care and central precocious puberty. Triptorelin is one of the most commonly used GnRH agonists globally, though it faces the same competitive pressure as other agents in this class from newer oral GnRH antagonists like relugolix, which avoid the initial hormone flare and offer potential cardiovascular advantages. Clinical data demonstrate reliable testosterone suppression comparable to other GnRH agonists in this class.
Evidence Reviews
Regulatory Status
Deep Dives
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
