Leuprolide
FDA-approved GnRH agonist — initial LH/FSH stimulation followed by HPG axis suppression via receptor downregulation.
Research facts
| Half-life | ~3 hours (daily) / months (depot formulation) |
|---|---|
| Route | SubQ / IM (depot) |
| Typical dose | 1 mg/day SubQ (prostate cancer) / 3.75–11.25 mg depot |
| Frequency | Daily SubQ or monthly/quarterly depot |
| Solvent | Commercial formulation |
| pH | N/A |
| Stability | Refrigerated |
Mechanism of action
Leuprolide is a synthetic GnRH agonist that, paradoxically, causes hormonal suppression via continuous stimulation. Physiological GnRH is released in pulses — continuous GnRH receptor stimulation causes receptor downregulation and desensitisation, leading to profound suppression of LH, FSH, and downstream sex hormones (testosterone, oestradiol). FDA-approved for prostate cancer, endometriosis, uterine fibroids, and precocious puberty. It is also used as "chemical castration" in sex offender management and as a puberty blocker in gender dysphoria management.
Documented effects (research-model)
- FDA-approved for prostate cancer (medical castration)
- FDA-approved for endometriosis (oestrogen suppression)
- FDA-approved for central precocious puberty
- Uterine fibroid treatment (oestrogen suppression)
- Research tool for HPG axis study
Research protocols
| Protocol | Dose | Frequency | Cycle | Vial |
|---|---|---|---|---|
| Prostate Cancer | 7.5 mg IM depot monthly | Monthly | Ongoing (cancer treatment) | Lupron Depot kit |
Research context only. Not medical advice. Consult a qualified healthcare professional before any protocol decision.
Synergies
No documented synergies in the current reference set.
Myths & misconceptions
Evidence gaps
- Long-term cognitive and cardiovascular effects of extended medical castration.
- Optimal cessation protocol for HPG axis recovery after prolonged use.
Safety notes
FDA-approved with extensive safety data. Hot flushes, bone density loss (long-term use), mood changes, cardiovascular risk with prolonged androgen deprivation. Medical supervision required. Not for research purposes beyond validated clinical indications.
Biomarkers to monitor
Primary-source citations
- PMID 8374620 — Leuprolide: clinical pharmacology and applications (Pharmacotherapy. 1993)
Frequently asked
What is Leuprolide?
Leuprolide (Lupron — GnRH Agonist for Hormonal Suppression) is a research compound classified in our library as Tier B — Some human data + strong preclinical evidence.. FDA-approved GnRH agonist — initial LH/FSH stimulation followed by HPG axis suppression via receptor downregulation.
What is the evidence tier for Leuprolide?
We classify Leuprolide as Tier B: Some human data + strong preclinical evidence. See our full peptide evidence tiers explainer for how we assign S/A/B/C/D.
What is the research dose of Leuprolide?
For Leuprolide, typical research dose is 1 mg/day SubQ (prostate cancer) / 3.75–11.25 mg depot, route is SubQ / IM (depot), half-life is ~3 hours (daily) / months (depot formulation). Protocols vary by research goal — see the protocols section on this page for standard and advanced dosing schedules. Research use only, not medical advice.
Is Leuprolide safe?
FDA-approved with extensive safety data. Hot flushes, bone density loss (long-term use), mood changes, cardiovascular risk with prolonged androgen deprivation. Research context only — no compound on this site is approved for human therapeutic use unless explicitly noted.