Leuprolide

Leuprorelin (INN outside the US), leuprolide acetate/mesylate; Lupron, Lupron Depot, Lupron Depot-PED, Eligard, Fensolvi, Camcevi (US); Prostap, Enantone, Lucrin, Procren (EU/UK/AU)

Sexual health, hormones & signalling

Awaiting medical reviewEN ES DE FR PT ZH+ Follow for updates

Note on this profile. Leuprolide is an approved prescription medicine in most countries, not a research-only compound. This page explains the published science. Use outside a prescription carries real risks discussed below, particularly prolonged hormone suppression from dosing errors.

Summary

Class: Synthetic GnRH (LHRH) agonist nonapeptide; native GnRH with D-leucine at position 6 and an ethylamide replacing the C-terminal glycine
Mechanism: After an initial surge, continuously occupies pituitary GnRH receptors and desensitises them, suppressing LH/FSH and so testosterone or oestrogen to castrate/post-menopausal levels
Routes studied: Daily subcutaneous injection; intramuscular depot (1-, 3-, 4-, 6-monthly); subcutaneous depot (Eligard, Fensolvi, Camcevi)
Dose range reported: Approved (prostate cancer): 1 mg SC daily; depot 7.5 mg/month, 22.5 mg/3 months, 30 mg/4 months, 45 mg/6 months (Lupron Depot, Eligard); Camcevi 42 mg/6 months. Endometriosis: 3.75 mg monthly or 11.25 mg/3 months, 6 months (12 with add-back). Fibroids: 3.75 mg monthly up to 3 months with iron. CPP: Lupron Depot-PED 7.5–15 mg monthly or 11.25/30 mg per 3 months; Fensolvi 45 mg/6 months. IVF down-regulation (off-label US, standard practice): 0.5–1 mg SC daily. Community use: rare
Half-life: ~3 hours (SC bolus); depots release over 1–6 months
Storage: Depot kits and Eligard: refrigerate (Eligard) or room temperature (Lupron Depot) per label; mix immediately before use. Daily 5 mg/mL vial: refrigerate, protect from light
Regulatory status: Approved medicine (US since 1985, EU, UK, AU, ZA and many others)

Doses are as reported in studies or by the community — never recommendations.

1What it is

Leuprolide was the first GnRH approved for prostate cancer (1985, as a daily injection) and has been one of the most widely used hormone-suppressing drugs for forty years. Like triptorelin, it is a modified version of the body's own GnRH, engineered to be stable and potent. Beyond prostate cancer it is approved for endometriosis, fibroids and central precocious puberty, and used off-label for IVF pituitary suppression, premenopausal breast cancer (approved for this in some countries), puberty suppression in gender-affirming care, and occasionally paraphilic disorders. In the US the brand name "Lupron" has become shorthand for the whole class.

2How it's thought to work

Flare then suppression. the first 1–2 weeks raise LH and testosterone (or oestradiol); by weeks 2–4 the pituitary becomes refractory and sex-steroid levels fall to castrate/post-menopausal range.

Reversible. hormone levels recover after the depot is exhausted, typically over 2–6 months, more slowly with age and long treatment.

Depot technology. Lupron Depot uses polymer microspheres injected IM; Eligard and Fensolvi use a liquid polymer that solidifies under the skin; Camcevi is a ready-to-use SC emulsion.

Continuous GnRH receptor stimulation at the pituitary. The first weeks raise LH and testosterone or oestradiol — the flare — then the receptor is withdrawn from the cell surface and sex hormones fall to castrate or post-menopausal levels.Schematic — not to scale

3What the research shows

Advanced prostate cancer

Daily leuprolide matched diethylstilboestrol for disease control with fewer cardiovascular deaths in the pivotal trial (Leuprolide Study Group 1984, NEJM). Adding flutamide to leuprolide modestly improved survival in metastatic disease (Crawford 1989, NEJM). Depot formulations achieve castrate testosterone in >90% of men within 4 weeks, with 1-, 3-, 4- and 6-month products shown equivalent. Intermittent versus continuous androgen deprivation did not prove non-inferior for survival in metastatic disease (Hussain 2013, NEJM; mixed ). [2][3]

Endometriosis

Depot leuprolide reduces pelvic pain and dysmenorrhoea; adding norethindrone or oestrogen/progestin "add-back" preserved bone density and allowed 12 months of treatment while maintaining pain relief (Hornstein 1998, Obstet Gynecol). [4]

Uterine fibroids

Three months of pre-operative leuprolide shrinks fibroids and corrects anaemia; benefits reverse within months of stopping, so it is used as a bridge to surgery (Friedman 1991, Obstet Gynecol and class evidence). [5]

Graded A/B

Central precocious puberty

The 3-month depot (11.25 or 30 mg) suppressed stimulated LH to prepubertal levels in most children over 6 months (Lee 2012, JCEM); 6-month Fensolvi showed similar suppression (open-label phase 3). [6]

IVF "long protocol"

Daily leuprolide from the mid-luteal phase prevents premature LH surges; compared with antagonist protocols it gives similar live-birth rates with more OHSS and longer stimulation (Al-Inany 2016, Cochrane). [7]

Graded A/B

Puberty suppression in transgender youth, breast cancer ovarian suppression, paraphilias

Class evidence (triptorelin and goserelin trials for breast cancer; cohort data for the others). Leuprolide is used interchangeably in practice but has fewer dedicated trials.

4Reported side effects and interactions

Literature-reported

Common (literature). hot flushes (>50%), reduced libido, erectile dysfunction, fatigue, mood change and depression, headache, injection-site pain or nodules, weight gain, muscle loss, gynaecomastia, vaginal dryness, bone density loss (~3% lumbar spine at 6 months for endometriosis dosing; partially reversible).

Serious / warnings. tumour flare (bone pain, urinary obstruction, spinal cord compression) in the first weeks; hyperglycaemia and diabetes; increased risk of myocardial infarction, stroke and sudden cardiac death (class warning); QT prolongation; pituitary apoplexy (rare); seizures (reports, mostly in children or those with predisposing conditions); idiopathic intracranial hypertension in children (label update 2022); psychiatric events in children (emotional lability, aggression); hypersensitivity including rare anaphylaxis; sterile abscess at injection site.

Community-reported

little community use; the main reports are from patients, not experimenters.

Interactions. QT-prolonging drugs; hyperprolactinaemic drugs; invalidates pituitary-gonadal testing during treatment and for months after.

Markers researchers commonly monitor

Per label and specialist practice:

Marker	Why it's watched
Testosterone (men)	target <50 ng/dL (ideally <20); checked at 1 month and periodically; also tracks recovery after stopping.
PSA	prostate cancer disease marker.
LH/FSH and oestradiol (women, children)	confirm suppression; a GnRH-stimulated LH test is the CPP standard.
Bone mineral density (DEXA)	baseline and after 6–12 months; the main long-term cost.
Fasting glucose, HbA1c, lipids	metabolic class effects.
Blood pressure, weight, waist	cardiovascular class warning.
ECG (QTc)	if on QT-prolonging drugs or with cardiac history.
Haemoglobin/ferritin	in fibroid use, where anaemia correction is the goal.
Height velocity and bone age (children)	the CPP outcomes that matter.

Free for everyone. Safety information is never behind a paywall.

5Reconstitution and handling

Depot kits are with the supplied and specific steps and injected immediately; Eligard must warm to room temperature and be mixed within the kit's time limit. The daily 5 mg/mL multi-dose vial is drawn at 0.2 mL (1 mg) with an insulin syringe; mg-to-mL confusion is the main error.

Open in calculator, pre-loaded →

6Commonly studied alongside

Triptorelin and nafarelin (same class, this batch), cetrorelix and ganirelix (antagonist alternatives), norethindrone acetate add-back (not a peptide), gonadorelin and HCG (axis-stimulating comparators), somatropin (combined with GnRH agonists in some short-stature protocols).

Informational cross-links. Not stack recommendations.

7Regulatory status by region

Region	Status (checked —)
United States	FDA-approved: Lupron Depot (prostate cancer, endometriosis, fibroids), Lupron Depot-PED and Fensolvi (CPP), Eligard and Camcevi (prostate cancer), leuprolide 1 mg/day injection. IVF and breast-cancer uses are off-label
European Union	Authorised nationally (Enantone, Lucrin, Procren, Eligard) for prostate cancer, endometriosis, fibroids, CPP and in several countries premenopausal breast cancer
United Kingdom	MHRA-licensed (Prostap SR/3, Staladex); prescription-only
Australia	TGA-approved (Lucrin, Eligard); S4
South Africa	SAHPRA-registered (Lucrin, Eligard); prescription-only
Sport	WADA S2: GnRH and its analogues, including leuprorelin, are prohibited in males

8Open questions

Long-term cardiovascular and metabolic consequences of androgen deprivation, and whether antagonists are safer.
Long-term bone and neurodevelopmental outcomes of puberty suppression.
Optimal add-back regimens to extend gynaecological use beyond 12 months.

9References

1The Leuprolide Study Group (1984). Leuprolide versus diethylstilbestrol for metastatic prostate cancer. N Engl J Med. PubMed
2Crawford ED et al. (1989). A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. PubMed · DOI
3Hussain M et al. (2013). Intermittent versus continuous androgen deprivation in prostate cancer. N Engl J Med. PubMed · DOI
4Hornstein MD et al. (1998). Leuprolide acetate depot and hormonal add-back in endometriosis: a 12-month study. Obstet Gynecol. PubMed · DOI
5Friedman AJ et al. (1991). Treatment of leiomyomata uteri with leuprolide acetate depot: a double-blind, placebo-controlled, multicenter study. Obstet Gynecol. PubMed
6Lee PA et al. (2012). Efficacy and safety of leuprolide acetate 3-month depot 11.25 milligrams or 30 milligrams for the treatment of central precocious puberty. J Clin Endocrinol Metab. PubMed · DOI
7Al-Inany HG et al. (2016). Gonadotrophin-releasing hormone antagonists for assisted reproductive technology. Cochrane Database Syst Rev. PubMed · DOI
8Lupron Depot / Eligard / Fensolvi prescribing information (current labels). PubMed

References are being resolved to PubMed/DOI identifiers; links search PubMed for the citation until then.

10Community

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Self-reported side effects Phase 2

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11Page history

26 Oct 2026Profile published — awaiting medical review

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