Leuprolide
FDA-approved GnRH agonistEstablished
FDA-approved GnRH agonist for prostate cancer, endometriosis, and central precocious puberty. Causes pituitary downregulation after an initial flare. WADA S2 (GnRH analogues).
For research use only.
Key Facts
- CAS
- 53714-56-0
- Molecular Weight (MW)
- 1209.4 g/mol (free base); 1269.4 g/mol (acetate)
- Half-life
- ~3 hours (immediate-release); depot provides sustained levels
- Unit
- mcg
- Administration Route
- Subcutaneous / Intramuscular
- Frequency
- Daily, monthly, every 3 months, or every 4 months depending on formulation
- Last updated
- 8/23/2026
- Targets
- GnRH receptor
Overview
FDA-approved GnRH agonist for prostate cancer, endometriosis, and central precocious puberty. Causes pituitary downregulation after an initial flare. WADA S2 (GnRH analogues).
Protocol
- Dosage Range
- Varies by indication: 1 mg daily, 7.5 mg monthly, 22.5 mg every 3 months, or 30 mg every 4 months
- Frequency
- Daily, monthly, every 3 months, or every 4 months depending on formulation
- Cycle
- Long-term use as prescribed
- Administration Route
- Subcutaneous / Intramuscular
- Reconstitution Guide
- Depot formulations require reconstitution per package insert
May vary by vendor concentration and protocol.
Science
Mechanism of Action
Continuous GnRH-receptor stimulation suppresses LH/FSH after the flare, lowering sex steroids. Depot formulations last 1โ6 months.
Targets
GnRH receptor
Studies
- Leuprolide androgen-deprivation therapyโ Journal/year not available
Benefits
Labeled hormone-dependent disease therapy
Potential Side Effects
- Hot flashes
- Bone loss
- Flare phenomenon
- Injection-site reactions
References
- FDA label โ Lupron DepotExternal link ยท Year โ
- WADA Prohibited List 2026External link ยท Year โ