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Hormonal & reproductive

Leuprolide

Also called leuprorelin, Lupron Depot, Eligard, Fensolvi, Camcevi

Leuprolide is a lab-made version of the brain hormone GnRH. Given continuously, it shuts down the body's production of testosterone or estrogen, so it is used for prostate cancer, endometriosis, fibroids and early puberty.

FDA-approvedApproved by the FDA for at least one use after large human trials.

All printable flashcards

Drawn from its published sequence: 9 residues, one bead each.

Overview

Leuprolide is a lab-made version of the brain hormone GnRH. Given continuously, it shuts down the body's production of testosterone or estrogen, so it is used for prostate cancer, endometriosis, fibroids and early puberty.

How it works

Established: leuprolide is a GnRH receptor agonist that is stronger than natural GnRH. At first it causes a short surge of LH, FSH and sex hormones (the 'flare'). With continuous exposure, the pituitary stops responding, LH and FSH fall, and testosterone drops to castrate levels within 2-4 weeks. The effect reverses when treatment stops (FDA label).

What research shows

  • Prostate cancer: 94% of men (51/54) reached castrate testosterone (≤50 ng/dL) within 30 days on 7.5 mg monthly; about 93% stayed suppressed from week 4 to 48 on 45 mg every 6 months (FDA label).
  • Expected testosterone flare in the first weeks can briefly worsen symptoms such as bone pain or urinary blockage (FDA label).

Doses studied in people

Study or labelDose usedSource
FDA label (Lupron Depot), advanced prostate cancer — 1-month7.5 mg intramuscularly every 4 weeks1
FDA label (Lupron Depot), advanced prostate cancer — 3-month22.5 mg intramuscularly every 12 weeks1
FDA label (Lupron Depot), advanced prostate cancer — 4-month30 mg intramuscularly every 16 weeks1
FDA label (Lupron Depot), advanced prostate cancer — 6-month45 mg intramuscularly every 24 weeks1

Depot strengths are not interchangeable; other leuprolide products (e.g., for endometriosis or early puberty) have different labeled doses.

Read this first: these are the amounts given to participants in published studies or written on official prescribing labels, reported for reference. They are not recommendations. Trial doses were chosen for specific patients under medical supervision, and a dose that is safe in one person can be harmful in another.

Weekly protocol

How the schedule looks week by week. Each chart says where it comes from: a prescribing label, a clinical trial, or a protocol commonly reported online.

Lupron Depot 1-month (prostate cancer)

Prescribing label

One week

D1D2D3D4D5D6D7

Once every 4 weeks · Intramuscular injection (depot)

Dose by week

7.5 mg every 4 weekswk 1+
Course
Ongoing
Note
For advanced prostate cancer. Depot strengths are not interchangeable; other leuprolide products have different labeled doses.
Source
LUPRON DEPOT prescribing information (FDA, 2025)

Lupron Depot 3-month (prostate cancer)

Prescribing label

One week

D1D2D3D4D5D6D7

Once every 12 weeks · Intramuscular injection (depot)

Dose by week

22.5 mg every 12 weekswk 1+
Course
Ongoing
Note
4-month (30 mg every 16 weeks) and 6-month (45 mg every 24 weeks) depots also exist.
Source
LUPRON DEPOT prescribing information (FDA, 2025)

Reference only, not a recommendation. Label and trial schedules were set for specific patients under medical supervision. Use the calculator only to understand the arithmetic.

Safety

  • Tumor flare: testosterone rises about 50% early on; watch for bone pain, nerve compression, urinary obstruction and spinal cord compression (FDA label).
  • Hyperglycemia and new or worsening diabetes; monitor glucose and lipids (FDA label).
  • Higher reported risk of heart attack, sudden cardiac death and stroke with GnRH agonists in men (FDA label).
  • QT prolongation with androgen deprivation; convulsions have been reported (FDA label).
  • Common: hot flashes/sweats, injection-site reactions, pain, fatigue, testicular atrophy (FDA label).
  • Embryo-fetal toxicity; long-term use lowers bone density (class effect of androgen deprivation).

Report side effects of any drug or product to the FDA through MedWatch. For a possible poisoning in the US, call Poison Control at 1-800-222-1222.

Storage and stability

Lupron Depot kits: store at 20-25°C (FDA label).

General lab handling, not instructions for personal use. See Storage and stability.

History

Leuprolide was one of the first long-acting GnRH agonists, developed after GnRH itself was identified in the early 1970s. The Lupron Depot sustained-release formulation was first approved in the US in 1989 for advanced prostate cancer. Later depot strengths allow dosing every 1, 3, 4 or 6 months, and other formulations treat endometriosis, uterine fibroids and central precocious puberty.

Common questions

Is leuprolide FDA-approved?

Yes. Lupron Depot was approved in 1989 for advanced prostate cancer, and other leuprolide products are approved for endometriosis, uterine fibroids and early puberty 1. It is prescription only and given by a healthcare provider 1.

How does leuprolide lower testosterone?

It first causes a short rise in sex hormones, called a 'flare' 1. With steady exposure the pituitary gland stops responding, and testosterone drops to castrate levels within 2 to 4 weeks 12.

What does the research show?

On the FDA label, 94% of men with prostate cancer reached castrate testosterone within 30 days on the 1-month depot 12. About 93% stayed suppressed from week 4 to 48 on the 6-month depot 12.

What doses are on the FDA label?

For advanced prostate cancer, the Lupron Depot label lists 7.5 mg every 4 weeks, 22.5 mg every 12 weeks, 30 mg every 16 weeks or 45 mg every 24 weeks, all by injection into muscle 1. These are labeled amounts for that use, and the depot strengths are not interchangeable 1.

What are the main side effects and risks?

Common effects include hot flashes, injection-site reactions, tiredness and testicle shrinkage 1. The label also warns about the early tumor flare, high blood sugar, and a higher reported risk of heart attack and stroke in men 1.

Is leuprolide banned in sport?

Yes, for male athletes. WADA's 2026 list prohibits it at all times in males as a testosterone-stimulating peptide and names leuprorelin as an example 90.

Sources

  1. LUPRON DEPOT (leuprolide acetate for depot suspension) prescribing information (2025) FDA label
  2. Lupron Depot prescribing information (clinical studies, mechanism) FDA label
  3. ChEBI: leuprolide (CHEBI:6427) Journal
  4. WADA 2026 Prohibited List Regulatory

Last reviewed 2026-10-25 · How we research · Found an error? See our corrections policy.