Leuprolide
Also known as: Leuprorelin, Lupron Depot, Eligard, Fensolvi, Camcevi
A GnRH agonist used to suppress sex hormones in prostate cancer, endometriosis, fibroids and central precocious puberty. FDA-approved prescription drug.
Last updated
Mechanism of Action
Leuprolide is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with higher potency and a longer half-life than the native hormone. It binds pituitary GnRH receptors and initially increases LH and FSH release, which causes a transient rise in testosterone or estradiol (the 'flare'). Continuous exposure then desensitizes and downregulates the receptors, so gonadotropin secretion falls and sex steroids drop to castrate or postmenopausal levels within about 2-4 weeks. Depot formulations release the drug over 1 to 6 months to maintain that suppression.
- Half-life
- ~3 hours (injection); depots release drug over 1-6 months
- Administration Routes
- Intramuscular, Subcutaneous
- Research Status
- Clinical
Reported Benefits
- Palliative treatment of advanced prostate cancer (androgen deprivation)
- Management of endometriosis pain and lesions
- Preoperative treatment of anemia from uterine fibroids, with iron
- Treatment of central precocious puberty in children
Potential Side Effects
- Hot flashes, sweating and decreased libido
- Transient tumor flare or symptom worsening in the first weeks
- Loss of bone mineral density with prolonged use
- Hyperglycemia and increased cardiovascular risk in men on androgen deprivation; QT prolongation
- Injection-site reactions; mood changes and, in children, psychiatric events and seizures
Common Dosing
Formulation determines the schedule: depot injections are given intramuscularly or subcutaneously once every 1, 3, 4 or 6 months depending on the product and indication, and a daily subcutaneous solution also exists. Gynecologic courses are time-limited because of bone loss, and pediatric doses are set by weight and product. Injections are given by or under the direction of a clinician. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Hypersensitivity to GnRH, GnRH agonists or any component
- Pregnancy
- Undiagnosed abnormal vaginal bleeding (gynecologic use)
No documented stacking partners for Leuprolide yet.
- View
Leuprolide versus diethylstilbestrol for metastatic prostate cancer
1984
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Randomized controlled trial of depot leuprolide in patients with chronic pelvic pain and clinically suspected endometriosis. Pelvic Pain Study Group
1999
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Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide Acetate Treatment for Central Precocious Puberty
2020