Last reviewed 2026-04-23 · How we verify

Leuprolide Acetate (LA)

Leuprolide acetate is a gonadotropin-releasing hormone (GnRH) agonist that suppresses luteinizing hormone and follicle-stimulating hormone, leading to decreased testosterone and estrogen production.

Leuprolide acetate is a gonadotropin-releasing hormone (GnRH) agonist that suppresses luteinizing hormone and follicle-stimulating hormone, leading to decreased testosterone and estrogen production. Used for Advanced prostate cancer, Endometriosis, Uterine fibroids.

At a glance

Mechanism of action

Leuprolide works by binding to GnRH receptors in the pituitary gland, initially causing a surge in LH and FSH (flare effect), followed by sustained suppression of these hormones through receptor desensitization. This results in castration-level testosterone suppression in males and estrogen suppression in females, making it effective for hormone-dependent conditions.

Approved indications

• Advanced prostate cancer
• Endometriosis
• Uterine fibroids
• Precocious puberty
• Breast cancer (premenopausal women)

Common side effects

• Hot flashes
• Injection site reaction
• Decreased libido
• Erectile dysfunction
• Headache
• Fatigue
• Bone pain (initial flare)
• Gynecomastia

Key clinical trials

• Treatment of High-Risk Prostate Cancer Guided by Novel Diagnostic Radio- and Molecular Tracers (PHASE2, PHASE3)
• A Study to Evaluate Leuprolide Acetate 45 mg 6-Month Formulation in Children With Central Precocious Puberty (CPP) (PHASE3)
• The Relation of GnRH Treatment to QTc Interval in Transgender Females
• Markers of Pubertal Suppression During Therapy for Precocious Puberty
• PROtecting Ovaries and Fertility During Chemotherapy - The PROOF Trial (PHASE3)

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.