Peptide LibraryLeuprolide
Also known as: Lupron, Eligard, Leuprorelin, GnRH agonist
Leuprolide (also called Lupron or Eligard) is an FDA-approved GnRH agonist. Leuprolide is a GnRH agonist with a D-leucine substitution at position six and an ethylamide C-terminus, changes that increase receptor affinity and greatly extend half-life relative to native GnRH.
For research use only.
Key Facts
- CAS
- 53714-56-0
- Molecular Weight (MW)
- 1209.4 g/mol (free base); 1269.4 g/mol (acetate)
- Half-life
- ~3 hours (immediate-release); depot provides sustained levels
- FDA status
- Approved
- Evidence level
- FDA Approved
- Human dose established
- Yes
- Administration Route
- Intramuscular · Subcutaneous
- Frequency
- Daily, monthly, every 3, 4 or 6 months, by product
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
- Targets
- GnRH receptor
Research summary
FDA-approved GnRH agonist for prostate cancer, endometriosis, and central precocious puberty. Causes pituitary downregulation after an initial flare. WADA S2 (GnRH analogues).
Research evidence
- Regulatory review (FDA label)9 reviewed sources
- Controlled human trialsNone in reviewed sources
- Early or uncontrolled human studiesNone in reviewed sources
- Lab & animal studiesNone in reviewed sources
How it works
Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess.
Peptide Library's Leuprolide profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Leuprolide dosage evidence
Leuprolide has FDA-approved human dosages that depend on the product, strength and indication. For advanced prostate cancer, LUPRON DEPOT (intramuscular) and ELIGARD (subcutaneous) give 7.5 mg every month, 22.5 mg every 3 months, 30 mg every 4 months or 45 mg every 6 months; CAMCEVI is 42 mg every 6 months, CAMCEVI ETM 21 mg every 3 months, and the daily injection is 1 mg. For endometriosis and fibroids, LUPRON DEPOT is 3.75 mg monthly or 11.25 mg every 3 months. For central precocious puberty, LUPRON DEPOT-PED is 7.5–15 mg monthly by weight, 11.25 or 30 mg every 3 months, or 45 mg every 6 months, and FENSOLVI is 45 mg every 6 months.
| Human dosing established | Yes |
|---|---|
| Route | Intramuscular · Subcutaneous |
| Frequency | Daily, monthly, every 3, 4 or 6 months, by product |
| Duration studied | Long-term for prostate cancer; up to 6 months per course for endometriosis; up to 3 months for fibroids; until the age of puberty for central precocious puberty |
| Titration | LUPRON DEPOT-PED monthly doses are chosen by body weight and raised to the next strength if suppression is not adequate. |
| Evidence level | FDA Approved |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| FDA label — LUPRON DEPOT, advanced prostate cancerFDA-approved label · FDA prescribing information | Men with advanced prostate cancer | 7.5 mg every 4 weeks, 22.5 mg every 12 weeks, 30 mg every 16 weeks or 45 mg every 24 weeks | Intramuscular | Every 4, 12, 16 or 24 weeks by strength | Long-term | Treatment of advanced prostate cancer | LUPRON DEPOT 7.5 mg, 22.5 mg, 30 mg and 45 mg (leuprolide acetate for depot suspension) — FDA prescribing information (AbbVie), DailyMed |
| FDA label — ELIGARD, advanced prostate cancerFDA-approved label · FDA prescribing information | Men with advanced prostate cancer | 7.5 mg every month, 22.5 mg every 3 months, 30 mg every 4 months or 45 mg every 6 months | Subcutaneous | Every 1, 3, 4 or 6 months by strength | Long-term | Treatment of advanced prostate cancer | ELIGARD (leuprolide acetate) for injectable suspension — FDA prescribing information (Tolmar), DailyMed |
| FDA label — CAMCEVI, advanced prostate cancerFDA-approved label · FDA prescribing information | Adults with advanced prostate cancer | 42 mg | Subcutaneous (prefilled syringe) | Once every 6 months | Long-term | Treatment of advanced prostate cancer | CAMCEVI (leuprolide) injectable emulsion — FDA prescribing information (Accord BioPharma), DailyMed |
| FDA label — CAMCEVI ETM, advanced prostate cancerFDA-approved label · FDA prescribing information | Adults with advanced prostate cancer | 21 mg | Subcutaneous (prefilled syringe) | Once every 3 months | Long-term | Treatment of advanced prostate cancer | CAMCEVI ETM (leuprolide) injectable emulsion — FDA prescribing information (Foresee), DailyMed |
| FDA label — leuprolide acetate injection (daily)FDA-approved label · FDA prescribing information | Men with advanced prostatic cancer (palliative treatment) | 1 mg (0.2 mL) | Subcutaneous | Once daily | Long-term | Palliative treatment of advanced prostatic cancer | Leuprolide acetate injection 1 mg/0.2 mL (Endo) — FDA prescribing information, DailyMed |
| FDA label — LUPRON DEPOT 3.75 mg, endometriosis and fibroidsFDA-approved label · FDA prescribing information | Women with endometriosis; women with anemia caused by uterine fibroids, before surgery, with iron therapy | 3.75 mg, alone or with norethindrone acetate 5 mg daily as add-back therapy (endometriosis) | Intramuscular | Once a month | Up to six injections for endometriosis; up to three months for fibroids. Total therapy with add-back should not exceed 12 months | Pain relief and reduction of endometriotic lesions; preoperative improvement of anemia | LUPRON DEPOT 3.75 mg (leuprolide acetate for depot suspension) — FDA prescribing information (AbbVie), DailyMed |
| FDA label — LUPRON DEPOT 11.25 mg, endometriosis and fibroidsFDA-approved label · FDA prescribing information | Women with endometriosis; women with anemia caused by uterine fibroids, before surgery, with iron therapy | 11.25 mg, alone or with norethindrone acetate 5 mg daily as add-back therapy (endometriosis) | Intramuscular | Once every 3 months | Up to two injections (6 months) for endometriosis; one injection for fibroids | Pain relief and reduction of endometriotic lesions; preoperative improvement of anemia | LUPRON DEPOT 11.25 mg (leuprolide acetate for depot suspension) — FDA prescribing information (AbbVie), DailyMed |
| FDA label — LUPRON DEPOT-PED, central precocious pubertyFDA-approved label · FDA prescribing information | Children with central precocious puberty | 1-month: 7.5 mg (25 kg or less), 11.25 mg (over 25 kg up to 37.5 kg) or 15 mg (over 37.5 kg). 3-month: 11.25 mg or 30 mg. 6-month: 45 mg | Intramuscular | Every month, every 12 weeks or every 24 weeks by formulation | Stopped at the appropriate age for the onset of puberty | Suppression of pituitary gonadotropins and sex steroids | LUPRON DEPOT-PED (leuprolide acetate for depot suspension) — FDA prescribing information (AbbVie), DailyMed |
| FDA label — FENSOLVI, central precocious pubertyFDA-approved label · FDA prescribing information | Children aged 2 and over with central precocious puberty | 45 mg | Subcutaneous | Once every 6 months | Stopped at the appropriate age for the onset of puberty | Suppression of pituitary gonadotropins and sex steroids | FENSOLVI (leuprolide acetate) for injectable suspension — FDA prescribing information (Tolmar), DailyMed |
Where sources disagree
- Depot strengths are not interchangeable. The LUPRON DEPOT labels say the strengths have different release characteristics, are not additive, and that a fractional dose or a combination of doses must not be used; a 3-month 11.25 mg depot is not three 3.75 mg monthly doses.
- The same strength can mean a different product and route: 7.5–45 mg LUPRON DEPOT is intramuscular, while ELIGARD and VABRINTY (Uronova; same four strengths and schedules), FENSOLVI and CAMCEVI are subcutaneous. LUTRATE DEPOT is a further 22.5 mg 3-month product for advanced prostate cancer.
- The prostate cancer labels warn of tumor flare in the first weeks of treatment (bone pain, urinary obstruction, spinal cord compression), and of hyperglycemia, diabetes and other metabolic changes with GnRH agonists. ELIGARD and CAMCEVI also warn of increased cardiovascular risk. The pediatric label warns of pseudotumor cerebri.
- Older DailyMed listings for VIADUR (Bayer, 2007) and the TAP LUPRON daily injection (2008) have not been updated since; the daily 1 mg injection is now listed by other labellers, including the Endo product cited here.
Handling & administration
- Reconstitution Guide
- Depot formulations require reconstitution per package insert
- Injection Sites
- Per product labeling
- Concentration Example
- Depot: 7.5 mg, 22.5 mg, or 30 mg per injection
- Timing Notes
- Inject subcutaneously or intramuscularly as per formulation
- Expected Onset
- Hormonal suppression typically achieved within 2-4 weeks
Sequence & molecular data
| Molecular formula | C59H84N16O12 |
|---|---|
| Molecular weight | 1209.4 g/mol (free base); 1269.4 g/mol (acetate) |
| CAS number | 53714-56-0 |
| Half-life | ~3 hours (immediate-release); depot provides sustained levels |
| Appearance | Solution and depot formulations |
| Formulation | Lyophilized Powder |
| PubChem CID | 657181 |
| FDA UNII | EFY6W0M8TG |
| ChEMBL | CHEMBL1201199 |
| DrugBank | DB00007 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Leuprolide is a GnRH agonist with a D-leucine substitution at position six and an ethylamide C-terminus, changes that increase receptor affinity and greatly extend half-life relative to native GnRH. Delivered continuously from a depot rather than in physiological pulses, it first stimulates the pituitary — the testosterone or oestrogen flare seen in the first one to two weeks — and then desensitises and downregulates the GnRH receptor. Gonadotropin secretion falls and sex steroid production drops to castrate concentrations within roughly two to four weeks. The initial flare is clinically relevant, which is why anti-androgen cover is used in advanced prostate cancer.
Origin
Synthetic nonapeptide GnRH analog.
Targets
Studies
- Treatment of High-Risk Biochemically Recurrent Prostate Cancer With Enzalutamide in Combination With Leuprolide: Secondary End Points From the EMBARK Trial
- Testosterone Recovery for Relugolix Versus Leuprolide in Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study
- Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized Trial
- Long-acting injectable PLGA/PLA depots for leuprolide acetate: successful translation from bench to clinic
- Improved Survival with Enzalutamide in Biochemically Recurrent Prostate Cancer
Research statistics
3,732 PubMed publications · 68.6% human clinical research · 380 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
Regulatory & research status
Leuprolide is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Availability | Prescription-Only |
| WADA (sport) | Banned in Sport |
| Library classification | FDA-Approved |
How FDA approval, compounding and research-only status differ
Benefits
Leuprolide side effects
The effects below are drawn from Leuprolide's prescribing information, which lists the full adverse-reaction data.
Side Effects
- Hot flashes
- Bone loss
- Flare phenomenon
- Injection-site reactions
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
Leuprolide: frequently asked questions
What is Leuprolide?
FDA-approved GnRH agonist for prostate cancer, endometriosis, and central precocious puberty. Causes pituitary downregulation after an initial flare. WADA S2 (GnRH analogues).
How does Leuprolide work?
Leuprolide is a GnRH agonist with a D-leucine substitution at position six and an ethylamide C-terminus, changes that increase receptor affinity and greatly extend half-life relative to native GnRH. Delivered continuously from a depot rather than in physiological pulses, it first stimulates the pituitary — the testosterone or oestrogen flare seen in the first one to two weeks — and then desensitises and downregulates the GnRH receptor.
Is Leuprolide FDA approved?
Yes. Leuprolide is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
What is the half-life of Leuprolide?
Reported half-life for Leuprolide is ~3 hours (immediate-release); depot provides sustained levels. Half-life describes how long the compound persists in circulation, not how long any effect lasts, and published figures vary with route of administration, formulation and the population studied.
Is Leuprolide banned in sport?
Leuprolide is recorded here as prohibited in sport. Athletes subject to anti-doping rules should check the current WADA Prohibited List directly, since it is revised annually and classifications change.
What peptides are similar to Leuprolide?
Compounds most often compared with Leuprolide include Goserelin, Triptorelin, Nafarelin and Histrelin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- FDA label — Lupron DepotExternal reference
- WADA Prohibited List 2026External reference
- Treatment of High-Risk Biochemically Recurrent Prostate Cancer With Enzalutamide in Combination With Leuprolide: Secondary End Points From the EMBARK Trial — J Urol, 2026External reference
- Testosterone Recovery for Relugolix Versus Leuprolide in Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study — Eur Urol Oncol, 2024External reference
- Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized Trial — Circulation, 2021External reference
- Long-acting injectable PLGA/PLA depots for leuprolide acetate: successful translation from bench to clinic — Drug Deliv Transl Res, 2023External reference
- Improved Survival with Enzalutamide in Biochemically Recurrent Prostate Cancer — N Engl J Med, 2026External reference
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Leuprolide profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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