Reproductive-axis (HPG) peptides
Leuprolide (Leuprorelin)
Also known as leuprorelin · Lupron · Eligard
A GnRH-agonist peptide that first stimulates, then shuts down, the reproductive axis — "medical castration" used in prostate cancer and other hormone-driven conditions.
In 60 seconds
Registered medicine (prostate cancer, endometriosis, central precocious puberty; also approved in Japan for spinal and bulbar muscular atrophy). Effects follow from sex-steroid suppression (hot flushes, bone loss); the initial flare is a recognised issue.
- Reviews leuprorelin as a GnRH analogue used across sex-hormone-related disorders.
- Describes how continued leuprorelin suppresses gonadal steroids and its depot pharmacokinetics.
- A meta-analysis of a 3-month leuprolide formulation in central precocious puberty.
Mechanism
Continuous exposure to a potent GnRH agonist desensitises pituitary GnRH receptors: after an initial LH/testosterone flare, gonadal steroid production is suppressed. Depot formulations deliver it over 1–6 months.
Research status
Registered medicine (prostate cancer, endometriosis, central precocious puberty; also approved in Japan for spinal and bulbar muscular atrophy).
Key studies
Reviews leuprorelin as a GnRH analogue used across sex-hormone-related disorders.
Leuprorelin. A review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disorders — Drugs, 1994 · PMID 7533699
Describes how continued leuprorelin suppresses gonadal steroids and its depot pharmacokinetics.
Clinical pharmacokinetics of depot leuprorelin — Clin Pharmacokinet, 2002 · PMID 12083977
A meta-analysis of a 3-month leuprolide formulation in central precocious puberty.
The Effect of Leuprolide Acetate 11.25 mg 3-Month Formulation in Children with Central Precocious Puberty: A Systematic Review and Meta-analysis — Adv Ther, 2025 · PMID 40498278
Reviews the polymer depot technology behind long-acting leuprolide.
Long-acting injectable PLGA/PLA depots for leuprolide acetate: successful translation from bench to clinic — Drug Deliv Transl Res, 2023 · PMID 35976565
Safety signals in the literature
Effects follow from sex-steroid suppression (hot flushes, bone loss); the initial flare is a recognised issue.
Legal status (South Africa)
Gonadotropins and GnRH analogues are scheduled prescription medicines in South Africa; research use only.
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Comparisons
Questions
What is Leuprolide (Leuprorelin)?
A GnRH-agonist peptide that first stimulates, then shuts down, the reproductive axis — "medical castration" used in prostate cancer and other hormone-driven conditions. Continuous exposure to a potent GnRH agonist desensitises pituitary GnRH receptors: after an initial LH/testosterone flare, gonadal steroid production is suppressed. Depot formulations deliver it over 1–6 months.
What is the research status of Leuprolide (Leuprorelin)?
Registered medicine (prostate cancer, endometriosis, central precocious puberty; also approved in Japan for spinal and bulbar muscular atrophy).
What safety signals are reported for Leuprolide (Leuprorelin)?
Effects follow from sex-steroid suppression (hot flushes, bone loss); the initial flare is a recognised issue.
Does Living Water Labs stock Leuprolide (Leuprorelin)?
Not at present. Leuprolide (Leuprorelin) is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Gonadotropins and GnRH analogues are scheduled prescription medicines in South Africa; research use only.
More in Reproductive axis
Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.
