ReproductiveFDA Approved

Leuprolide (Lupron)

Subcutaneous injection, Intramuscular injection (depot)

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)

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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.