Last reviewed 2026-04-20 · How we verify

Lupron (leuprolide)

Lupron works by binding to and activating the gonadotropin-releasing hormone receptor, which ultimately leads to a decrease in the production of sex hormones.

Lupron (leuprolide) is a small molecule gonadotropin-releasing hormone receptor agonist developed by Accord Healthcare S.L.U. and approved by the FDA in 1985. It targets the gonadotropin-releasing hormone receptor to treat various conditions, including advanced prostatic carcinoma, anemia due to bleeding uterine leiomyoma, endometriosis, and precocious puberty. As an off-patent medication, Lupron is available from its current owner, Accord, without any active Orange Book patents. Key safety considerations include its potential impact on bone density and the risk of injection site reactions. Lupron's commercial status as an off-patent medication allows for generic manufacturers to produce the medication.

At a glance

Mechanism of action

Leuprolide acetate, GnRH agonist, acts as potent inhibitor of gonadotropin secretion (LH and follicle stimulating hormone (FSH)) when given continuously in therapeutic doses. Following an initial stimulation of GnRH receptors, chronic administration of leuprolide acetate results in downregulation of GnRH receptors, reduction in release of LH, FSH and consequent suppression of ovarian and testicular production of estradiol and testosterone respectively. This inhibitory effect is reversible upon discontinuation of drug therapy.

Approved indications

• Advanced Prostatic Carcinoma
• Anemia due to Bleeding Uterine Leiomyoma
• Endometriosis
• Precocious puberty

Common side effects

• Intercepted product preparation error
• Syringe issue
• Device leakage
• Wrong technique in product usage process
• Prostatic specific antigen increased
• Intercepted medication error
• Hot flush
• Product physical consistency issue
• Blood testosterone abnormal
• Prostate cancer metastatic
• Product leakage
• Blood testosterone increased

Key clinical trials

• A Single-Arm Phase II Study of Neoadjuvant Intensified Androgen Deprivation (Leuprolide and Abiraterone Acetate) in Combination With AKT Inhibition (Capivasertib) for High-Risk Localized Prostate Cancer With PTEN Loss (PHASE2)
• Exploration of Treatment Effect of Novel Hormone Therapy Combined With Local Treatment Based on PSMA PET/CT Evaluation in mHSCP Patients (PHASE2)
• Gonadotropin-releasing Hormone Agonist (GnRHa) in Ovarian Preservation in SLE Subjects Receiving Cyclophosphamide as Determined by Questionnaires
• Testing the Addition of Darolutamide to Hormonal Therapy (Androgen Deprivation Therapy [ADT]) After Surgery for Men With High-Risk Prostate Cancer, The ERADICATE Study (PHASE3)
• Study to Test the Drug Darolutamide Along With the Drugs Leuprolide Acetate and Exemestane in Patients With Recurrent Ovarian Granulosa Cell Tumors (PHASE2)
• Treatment of High-Risk Prostate Cancer Guided by Novel Diagnostic Radio- and Molecular Tracers (PHASE2,PHASE3)
• Neoadjuvant ADT + Darolutamide With Pembrolizumab, Followed by Adjuvant Pembrolizumab in Molecularly Stratified High-Risk Prostate Cancer (PHASE2)
• Neoadjuvant Endocrine Therapy, Palbociclib, Avelumab in Estrogen Receptor Positive Breast Cancer (PHASE2)

Primary sources

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