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ReproductiveFDA Approved

Leuprolide (Lupron)

Subcutaneous injection, Intramuscular injection (depot)
Written by Peptide Association Editorial TeamMedically reviewed by Ian Justl Ellis, MD, CPTLast reviewed Editorial policy

Overview

A synthetic nonapeptide GnRH agonist approximately 15-fold more potent than native GnRH. After an initial stimulatory phase (flare effect) lasting 1-2 weeks, chronic leuprolide administration downregulates pituitary GnRH receptors, resulting in profound suppression of LH, FSH, and downstream sex steroids.

Mechanism of Action

This chemical castration effect is exploited in treating hormone-sensitive cancers, endometriosis, and precocious puberty.

Research Summary & Key Findings

FDA-approved for prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and as part of IVF protocols. Depot formulations available for 1-, 3-, 4-, and 6-month dosing intervals. In prostate cancer, achieves castrate testosterone levels in >95% of patients. EMBARK trial (2023) demonstrated benefit in biochemically recurrent prostate cancer.

Clinical Status

FDA Approved

Leuprolide (Lupron) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Administration Routes

Subcutaneous injectionIntramuscular injection (depot)

References

Primary literature

Study-level citations for this compound are being verified against the primary sources before publication. The database queries above return the current indexed literature in the meantime.

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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol. See our editorial policy for how this content is produced and reviewed.