← All compounds · evidence tier first, by design

Evidence tier for each claimed use · ← established · unknown →
Use	E2	E3	E4
E2 Advanced prostate cancer (androgen deprivation)	E2
E2 Endometriosis (pain)	E2
E3 Uterine leiomyomata (fibroids), before surgery		E3
E4 Central precocious puberty			E4

Class A · Approved

Leuprorelin

Synthetic GnRH agonist nonapeptide: pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt (N-terminal pyroglutamate, D-leucine at position 6, C-terminal ethylamide); no standard one-letter sequence is given.

Non-standard residues or modifications: no plain one-letter sequence

Also: Leuprolide, Leuprolide acetate, Leuprorelin mesilate · Brands: Lupron Depot, Lupron, Camcevi

A synthetic nine-residue analogue of gonadotropin-releasing hormone (GnRH). After an initial surge, continued exposure suppresses pituitary gonadotropin release and lowers testosterone or oestrogen to castrate or postmenopausal levels. It is an approved prescription drug in long-acting injectable forms. Labelled uses include advanced prostate cancer, endometriosis, uterine fibroids (with iron, before surgery) and central precocious puberty, varying by product and jurisdiction.

US A approved
EU A approved
UK ? not verified
CA A approved
AU ? not verified
JP ? not verified
CN ? not verified

01Regulatory status, by jurisdiction

Jurisdiction	Status	Detail and primary source
US	Approved	Lupron Depot (NDA 019732, AbbVie Endocrine Inc) is listed in Drugs@FDA with marketing status Prescription and original approval on 26 January 1989; further Lupron Depot strengths are under NDA 020517. “01/26/1989 ORIG-1 Approval Type 3 - New Dosage Form PRIORITY” Drugs@FDA: FDA-Approved Drugs - NDA 019732 (Lupron Depot) · retrieved 2026-10-10
EU	Approved	Camcevi (leuprorelin mesilate, EMEA/H/C/005034) is centrally authorised for hormone-dependent prostate cancer; marketing authorisation issued 24 May 2022. Other leuprorelin products in the EU are nationally authorised and were not individually verified. “Camcevi is indicated for the treatment of hormone dependent advanced prostate cancer and for the treatment of high-risk localised and locally advanced hormone dependent prostate cancer in combination with radiotherapy.” Camcevi \| European Medicines Agency (EMA) · retrieved 2026-10-10
CA	Approved	Health Canada Drug Product Database lists Lupron Depot (AbbVie Corporation) with current status Marketed. “Current status: Marketed Current status date: 2013-12-11 Original market date: See footnote 1 1989-12-31 Product name: LUPRON DEPOT” Drug Product Database: Product information - LUPRON DEPOT · retrieved 2026-10-10
UK AU JP CN	Not yet verified from a primary source. No status is shown rather than an unsourced one.

Sport (WADA): Prohibited · class S2.2.1. “S2.2.1 TESTOSTERONE-STIMULATING PEPTIDES IN MALES INCLUDING, BUT NOT LIMITED TO: chorionic gonadotrophin (CG) luteinizing hormone (LH) gonadotrophin- releasing hormone (GnRH, gonadorelin) and its agonist analogues (e.g. buserelin, deslorelin, goserelin, histrelin, leuprorelin, nafarelin and triptorelin)” WADA source

02What the human evidence shows

Advanced prostate cancer (androgen deprivation)

1published human RCTs

1published human trials

272registered studies

110with posted results

A randomised trial in metastatic prostate cancer compared leuprolide with diethylstilbestrol, the hormonal standard of the time, and reported similar disease response with fewer cardiovascular and breast adverse effects. The wider GnRH-agonist trial literature is larger than the single RCT cited here; only the verified trial is counted.

[1] Comparable response rates with leuprolide and diethylstilbestrol in men with metastatic prostate cancer, with fewer cardiovascular and breast adverse effects in the leuprolide arm

Registered-study counts: ClinicalTrials.gov intervention search “leuprolide prostate cancer”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.

Endometriosis (pain)

2published human RCTs

2published human trials

31registered studies

8with posted results

A randomised, double-blind, placebo-controlled trial reported reduced endometriosis-associated pain with depot leuprolide. A 12-month randomised trial tested hormonal add-back regimens alongside leuprolide to limit bone loss and menopausal symptoms. Hypo-oestrogenic adverse effects, including bone mineral density loss, limit duration of use.

[2] Greater reduction in endometriosis symptoms with depot leuprolide than with placebo in a randomised double-blind trial
[3] Randomised comparison of hormonal add-back regimens given with depot leuprolide in women with endometriosis, assessing pain relief and bone mineral density

Registered-study counts: ClinicalTrials.gov intervention search “leuprolide endometriosis”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.

Uterine leiomyomata (fibroids), before surgery

1published human RCTs

1published human trials

13registered studies

4with posted results

A small randomised, placebo-controlled, double-blind trial reported reductions in uterine and fibroid volume with depot leuprolide. Larger trials with surgical or long-term outcomes were not verified for this record.

[4] Reduction in uterine volume with depot leuprolide compared with placebo in women with uterine leiomyomata

Registered-study counts: ClinicalTrials.gov intervention search “leuprolide leiomyoma”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.

Central precocious puberty

No randomised controlled trial in humans has been published for this use.

0published human RCTs

1published human trials

23registered studies

10with posted results

Approval and current evidence in central precocious puberty rest on single-arm, open-label studies measuring suppression of the pituitary-gonadal axis, such as a recent phase 3 study of a long-acting formulation. A randomised placebo-controlled design is not used in this condition; no RCT is cited.

[5] Single-arm phase 3 study reporting suppression of luteinising hormone in children with central precocious puberty

Registered-study counts: ClinicalTrials.gov intervention search “leuprolide precocious puberty”, fetched 2026-10-10. Registered studies include trials of other uses; the gap between registered and reported is itself a finding.

03Safety signals

S1Large long-term human exposure (post-marketing surveillance)

Diabetes and cardiovascular disease during androgen deprivation [6]
In a large observational cohort of men with prostate cancer, GnRH-agonist therapy was associated with higher risk of incident diabetes, coronary heart disease, myocardial infarction and sudden cardiac death.
Bone mineral density loss with hypo-oestrogenism [3]
Bone loss during leuprolide treatment for endometriosis was the reason hormonal add-back regimens were tested in a randomised trial.

04What is unknown

The single prostate cancer RCT cited predates modern trial registration; registered-trial denominators for leuprolide will undercount the pre-2000 evidence base
Long-term outcomes of childhood treatment for central precocious puberty (adult height, fertility, bone health) are not established by the single-arm study cited
Whether the cardiometabolic associations seen in observational androgen-deprivation cohorts are causal has not been established by randomised data cited here
Status in the UK, Australia, Japan and China was not verified from regulator sources for this record

05Product quality

No independent purity results have been published for this compound yet. The purity programme will publish full methods and vendor-named results, passes and failures, once its protocol has had legal review.

06Citations

Leuprolide versus Diethylstilbestrol for Metastatic Prostate Cancer (1984). doi:10.1056/nejm198411153112004
Lupron depot (leuprolide acetate for depot suspension) in the treatment of endometriosis: a randomized, placebo-controlled, double-blind study (1990). doi:10.1016/s0015-0282(16)53755-8
Leuprolide Acetate Depot and Hormonal Add-Back in Endometriosis: A 12-Month Study (1998). doi:10.1016/s0029-7844(97)00620-0
A randomized, placebo-controlled, double-blind study evaluating the efficacy of leuprolide acetate depot in the treatment of uterine leiomyomata (1989). doi:10.1016/s0015-0282(16)60486-7
Long-term Safety, Efficacy, and PROs: Phase 3 Study of Leuprolide Acetate 6-month IM Depot in Central Precocious Puberty (2026). doi:10.1210/jendso/bvaf224
Diabetes and Cardiovascular Disease During Androgen Deprivation Therapy for Prostate Cancer. doi:10.1200/JCO.2006.06.2497

Every DOI is resolved against Crossref and every NCT number against ClinicalTrials.gov, title for title, before publication. Regulatory sources are cited inline above with a verbatim quote and retrieval date.

07Mechanism

Leuprolide is a GnRH receptor agonist; in human studies continuous exposure, after an initial rise, down-regulates pituitary GnRH receptors and suppresses luteinising hormone, follicle-stimulating hormone and sex-steroid levels.

Mechanism is placed last on purpose: a plausible mechanism is not evidence that a compound works in people.

Reviewed by OSMF research team (AI-assisted, source-verified) on 2026-10-10. Found an error? It goes in the corrections log: report it.