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).

Calculate Dose

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 1โ€“6 months.

Targets

GnRH receptor

Studies

Benefits

Labeled hormone-dependent disease therapy

Potential Side Effects

  • Hot flashes
  • Bone loss
  • Flare phenomenon
  • Injection-site reactions

References

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