Leuprolide

FDA Approved

Also known as: Lupron, Eligard, Leuprorelin

GnRH Agonist

Last reviewed: April 28, 2026

A synthetic GnRH agonist that paradoxically suppresses gonadotropin release with chronic use. One of the most commercially important peptide drugs, used in prostate cancer, endometriosis, precocious puberty, and fertility treatments.

Mechanism of Action

Initially stimulates LH and FSH release (flare effect), then downregulates GnRH receptors with continuous exposure, leading to profound suppression of testosterone and estrogen production. This 'chemical castration' effect is therapeutically useful.

Common Uses

  • Prostate cancer treatment
  • Endometriosis
  • Uterine fibroids
  • Precocious puberty
  • Fertility treatments (IVF protocols)

Known Risks

  • Hot flashes
  • Bone density loss with long-term use
  • Mood changes and depression
  • Initial testosterone flare (prostate cancer)
  • Injection site reactions
  • Cardiovascular risk with prolonged use

Regulatory Status

FDA Approved

FDA-approved as Lupron/Lupron Depot (multiple indications since 1985) and Eligard. One of the highest-revenue peptide drugs historically. Available in 1-month, 3-month, 4-month, and 6-month depot formulations.

Common Protocols

Protocol information is for educational reference only. Dosing varies significantly by individual, condition, and physician guidance. Always work with a licensed healthcare provider.

Intramuscular / Subcutaneous depot injection

Typical Dose

3.75–45 mg depot (varies by formulation)

Frequency

Monthly, quarterly, or semi-annually

Cycle Length

Duration depends on indication

Depot formulations provide sustained release. Initial flare effect requires awareness in prostate cancer patients. Monitor bone density with long-term use.

Related Compounds

Research References

This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before starting any peptide therapy. Data is compiled from published research and regulatory sources and may not reflect the most recent developments.