Leuprolide (Lupron)
GnRH Agonist / Hormonal TherapyapprovedAlso known as: Lupron, Lupron Depot, Leuprorelin, Eligard, Viadur
A synthetic GnRH agonist that, through continuous administration, paradoxically suppresses gonadotropin secretion and sex hormone production, used for prostate cancer, endometriosis, precocious puberty, and uterine fibroids.
Overview
Leuprolide (brand name Lupron) is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) that is approximately 80 times more potent than natural GnRH. When given continuously (rather than in the natural pulsatile pattern), leuprolide initially stimulates then profoundly suppresses pituitary LH and FSH secretion through receptor downregulation and desensitization — a process called 'medical castration.' This results in dramatic suppression of testosterone (in males) or estrogen (in females) to castrate levels within 2-4 weeks. It is one of the most widely prescribed hormonal therapies worldwide, available in daily, monthly, 3-month, 4-month, and 6-month depot formulations. Approved indications include advanced prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and as part of assisted reproduction protocols.
Mechanism of Action
Leuprolide acts as a GnRH superagonist with paradoxical suppressive effects: (1) Initially stimulates GnRH receptors causing a transient 'flare' of LH, FSH, and sex hormones (days 1-14); (2) Continuous receptor stimulation causes GnRH receptor downregulation and pituitary desensitization; (3) LH and FSH secretion drops to castrate levels by 2-4 weeks; (4) Testosterone (males) or estrogen (females) falls to castrate/menopausal levels; (5) D-Leu substitution at position 6 and ethylamide C-terminus increase receptor affinity and resist enzymatic degradation; (6) Depot formulations use biodegradable microspheres for sustained release over weeks to months.
Molecular Formula
C59H84N16O12
Molecular Weight
1209.40 g/mol
Sequence
pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt
Dosage Protocols
Dose Range
7.5mg – 45mg
Frequency
Monthly to every 6 months
Route
intramuscular / subcutaneous depot
Cycle Length
Ongoing
7.5mg monthly, 22.5mg every 3 months, 30mg every 4 months, or 45mg every 6 months. Anti-androgen co-administration for first 2 weeks to cover testosterone flare.
Source: FDA prescribing information
🧮 Personalized Dosage Calculator
💰 Estimated Pricing
Typical Supply
3.75mg or 7.5mg depot injection
Last Updated
2026-02
Brand Lupron. Monthly or 3-month depot. For prostate cancer, endometriosis, precocious puberty. Insurance usually covers.
⚠️ Prices are estimates based on publicly available data and may vary significantly by vendor, location, and prescription status. This is not medical or financial advice.
Side Effects
| Effect | Severity |
|---|---|
| Hot flashes | moderate |
| Bone density loss | severe |
| Initial disease flare | severe |
| Sexual dysfunction | moderate |
| Mood changes / Depression | moderate |
| Injection site reactions | mild |
Pros & Cons
Non-surgical alternative to orchiectomy for prostate cancer — reversible chemical castration
Long-acting depot formulations (up to 6 months) reduce treatment burden
Proven efficacy across multiple hormone-dependent conditions
Decades of clinical experience with well-characterized safety profile
Initial disease flare can be dangerous in prostate cancer (bone pain, spinal cord compression)
Bone density loss limits treatment duration for benign conditions
Significant quality of life impact from sex hormone suppression (hot flashes, sexual dysfunction, mood)
Expensive — depot formulations cost $1,000-5,000+ per injection
Research Studies
🩸 Blood Work
No specific bloodwork requirements reported for this peptide. General health panels are always recommended before starting any peptide protocol.
Legal Status
FDA-approved for prostate cancer, endometriosis, uterine fibroids, central precocious puberty, and assisted reproduction. Prescription-only. Available as daily SC injection, monthly/multi-month IM depot, and subcutaneous implant.
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