Leuprolide

approved

Also known as: Lupron, Leuprorelin, Eligard

Leuprolide is a synthetic gonadotropin-releasing hormone (GnRH) agonist that acts as a potent suppressor of the hypothalamic-pituitary-gonadal axis. Upon initial administration, it stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, causing a transient rise in sex steroids (testosterone or estradiol). With continuous exposure, however, leuprolide downregulates pituitary GnRH receptors, leading to a sustained suppression of gonadotropin secretion and subsequent reduction of gonadal steroid production to castrate levels. This paradoxical inhibitory effect forms the basis for its therapeutic utility in hormone-sensitive conditions. Key research findings from over 2,300 PubMed-indexed studies demonstrate leuprolide's efficacy in reducing testosterone levels in prostate cancer patients, with clinical trials showing improved progression-free survival when used as androgen deprivation therapy. In endometriosis, it alleviates pain and reduces lesion size by inducing a hypoestrogenic state. For central precocious puberty, leuprolide effectively halts or reverses premature sexual development by suppressing the pubertal hormonal axis. Long-term safety data indicate manageable adverse effects related to hypoestrogenism or hypogonadism, such as hot flashes, bone density loss, and mood changes. Clinically, leuprolide is approved for advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. Its depot formulations (e.g., monthly or quarterly injections) enable sustained drug release, improving patient adherence. While highly effective, its use requires monitoring for cardiovascular risk and bone health in prolonged therapy. For research purposes only — not medical advice.

Key data

Category
Hormonal & Endocrine
Molecular weight
1209.4 g/mol
Molecular formula
C59H84N16O12
CAS number
53714-56-0
Administration
subcutaneous, intramuscular
Research status
approved
References
2,332
Tags
gnrh-agonist, approved, oncology

Research & studies

Improved Survival with Enzalutamide in Biochemically Recurrent Prostate Cancer
The New England journal of medicine · 2026 · PubMed

Enzalutamide plus leuprolide reduced the risk of death by 40% versus leuprolide alone (HR 0.60, 95% CI 0.44-0.80, P<0.001).; 8-year overall survival was 78.9% with combination therapy vs 69.5% with leuprolide alone.; Enzalutamide monotherapy did not significantly improve overall survival compared to leuprolide alone (HR 0.83, 95% CI 0.63-1.10, P=0.19).; Safety findings were consistent with the primary metastasis-free survival analysis.

Enzalutamide with or without leuprolide in patients with high-risk biochemically recurrent prostate cancer: EMBARK post hoc analysis by age
European journal of cancer (Oxford, England : 1990) · 2026 · PubMed
Impact of treatment suspension on health-related quality of life in the EMBARK trial: a post hoc analysis
EClinicalMedicine · 2025 · PubMed
Effects of Enzalutamide on the Sexual Activity of Patients with Biochemically Recurrent Prostate Cancer: A Post Hoc Analysis of Patient-reported Outcomes in the EMBARK Study
European urology · 2025 · PubMed
Testosterone Recovery for Relugolix Versus Leuprolide in Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study
European urology oncology · 2024 · PubMed
Impact of Relugolix Versus Leuprolide on the Quality of Life of Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study
European urology · 2023 · PubMed
Improved Outcomes with Enzalutamide in Biochemically Recurrent Prostate Cancer
The New England journal of medicine · 2023 · PubMed

Enzalutamide plus leuprolide reduced risk of metastasis or death by 58% vs leuprolide alone (HR 0.42, 95% CI 0.30-0.61, p<0.001).; Enzalutamide monotherapy reduced risk of metastasis or death by 37% vs leuprolide alone (HR 0.63, 95% CI 0.46-0.87, p=0.005).; No substantial between-group differences in quality-of-life measures were observed.; Safety profile of enzalutamide was consistent with prior studies.

Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: A systematic review and network meta-analysis
Medicine · 2023 · PubMed

Frequently asked questions

What is Leuprolide?

Leuprolide is a synthetic gonadotropin-releasing hormone (GnRH) agonist that acts as a potent suppressor of the hypothalamic-pituitary-gonadal axis. Upon initial administration, it stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, causing a transient rise in sex steroids (testosterone

How does Leuprolide work?

GnRH agonist that suppresses gonadotropin and sex-steroid production after initial stimulation; used in prostate cancer, endometriosis, and precocious puberty.

What is the research status of Leuprolide?

Leuprolide is currently classified as approved, with 2,332 research references on record. This is for research purposes only and is not medical advice.

What is the molecular weight of Leuprolide?

Leuprolide has a molecular weight of approximately 1209.4 g/mol (formula C59H84N16O12).

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