Approved & therapeutic
Leuprolide
Lupron Depot, Eligard, Camcevi
Leuprolide is a synthetic GnRH agonist used for advanced prostate cancer, endometriosis, uterine fibroids and central precocious puberty. Despite being an agonist, its sustained action suppresses the reproductive axis, which is the therapeutic effect.
Also known as: Lupron, Lupron Depot, Eligard, Camcevi, Leuprorelin
- Status
- Leuprolide is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- The peptide itself has a short half-life of about 3 hours, but depot formulations sustain exposure over 1 to 6 months depending on the product.
- How it's taken
- Intramuscular or subcutaneous depot injection, or subcutaneous implant
- Mechanism
- Reproductive axis (GnRH / kisspeptin / oxytocin)
- Pathways
- GnRH, Androgen, Estrogen
How Leuprolide works
Normal GnRH release is pulsatile, and the pituitary requires that pulsatility to keep releasing LH and FSH. Continuous exposure to a GnRH agonist first causes a surge in LH, FSH and sex hormones, then downregulates and desensitises pituitary GnRH receptors, producing profound suppression of testosterone or estradiol within two to four weeks. That initial surge is the clinically important "flare" phenomenon.
What research has looked at
- Achieves medical castration in advanced prostate cancer, with testosterone suppression comparable to surgical orchiectomy.
- Suppresses estradiol in endometriosis and uterine fibroids, reducing lesion-associated pain and fibroid volume; treatment duration is limited by bone loss.
- Halts premature pubertal progression in central precocious puberty and preserves adult height potential.
- Depot formulations allow dosing at 1, 3, 4 or 6-month intervals depending on product.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- The initial testosterone or estradiol surge can transiently worsen disease — in prostate cancer this can cause bone pain, urinary obstruction or spinal cord compression, which is why an antiandrogen is often given during initiation.
- Hypogonadal effects: hot flashes, decreased libido, erectile dysfunction, fatigue and mood changes.
- Loss of bone mineral density with prolonged use; this limits the duration of therapy in benign gynaecological indications, often with add-back hormone therapy.
- Metabolic effects in prostate cancer including insulin resistance, altered lipids and increased cardiovascular risk with long-term androgen deprivation.
- Injection-site reactions, and convulsions have been reported.
Sources
- FDA approved-drug listing for leuprolide · U.S. Food & Drug Administration
- DailyMed prescribing information for leuprolide · NIH · DailyMed
- PubMed research on leuprolide GnRH agonist flare · NIH · National Library of Medicine
- DrugBank record for leuprolide · DrugBank
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Leuprolide FAQ
What is Leuprolide?
Leuprolide is a synthetic GnRH agonist used for advanced prostate cancer, endometriosis, uterine fibroids and central precocious puberty. Despite being an agonist, its sustained action suppresses the reproductive axis, which is the therapeutic effect.
How does Leuprolide work?
Normal GnRH release is pulsatile, and the pituitary requires that pulsatility to keep releasing LH and FSH. Continuous exposure to a GnRH agonist first causes a surge in LH, FSH and sex hormones, then downregulates and desensitises pituitary GnRH receptors, producing profound suppression of testosterone or estradiol within two to four weeks. That initial surge is the clinically important "flare" phenomenon.
Is Leuprolide FDA approved?
Yes. Leuprolide is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Leuprolide?
Reported half-life: The peptide itself has a short half-life of about 3 hours, but depot formulations sustain exposure over 1 to 6 months depending on the product.
How is Leuprolide taken?
Intramuscular or subcutaneous depot injection, or subcutaneous implant.
What side effects have been reported with Leuprolide?
Reported in the sources: The initial testosterone or estradiol surge can transiently worsen disease — in prostate cancer this can cause bone pain, urinary obstruction or spinal cord compression, which is why an antiandrogen is often given during initiation; Hypogonadal effects: hot flashes, decreased libido, erectile dysfunction, fatigue and mood changes; Loss of bone mineral density with prolonged use; this limits the duration of therapy in benign gynaecological indications, often with add-back hormone therapy; Metabolic effects in prostate cancer including insulin resistance, altered lipids and increased cardiovascular risk with long-term androgen deprivation; Injection-site reactions, and convulsions have been reported.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.