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Leuprolide

Lupron · Leuprorelin · Eligard

Hormonal AxisApproved

MW: 1209.4g/mol
Formula: C59H84N16O12

Leuprolide is a synthetic peptide classified as a gonadotropin-releasing hormone (GnRH) agonist, originally developed for the management of hormone-sensitive conditions such as prostate cancer. Researchers primarily study leuprolide for its role in androgen deprivation therapy, particularly in advanced prostate cancer cases. Key findings from clinical trials indicate that leuprolide, when combined with other agents like enzalutamide, can significantly improve metastasis-free survival compared to monotherapy. Additionally, studies suggest that while leuprolide effectively suppresses testosterone levels, newer agents like relugolix may offer advantages in terms of rapid testosterone suppression and reduced cardiovascular risks. Current research continues to explore leuprolide's efficacy and safety in various treatment combinations and settings.

Chemical Profile

Chemical Structure

Formula	C59H84N16O12
Molecular Weight	1209.4 g/mol
CAS Number	53714-56-0
PubChem CID	657181

Half-Life

SCSubcutaneous

~3 to 4 hours

IMIntramuscular

~3 to 4 hours

INIntranasal

Not applicable

POOral

Poor bioavailability

Leuprolide is often formulated in depot preparations for extended release.

Mechanism

Mechanism of Action

Leuprolide is a synthetic analog of gonadotropin-releasing hormone (GnRH) that acts as a GnRH agonist, binding to GnRH receptors in the pituitary gland, leading to an initial surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, followed by downregulation of these receptors and subsequent suppression of testosterone synthesis in the testes via the hypothalamic-pituitary-gonadal (HPG) axis. This action inhibits the signaling pathways associated with testosterone production, ultimately resulting in decreased androgen levels, which is critical for the treatment of hormone-sensitive prostate cancer. The exact molecular mechanisms underlying the long-term effects of leuprolide on prostate cancer progression are not fully understood.

Research

80 Research Publications

4,934

Total Citations

Human/RCT

6.1

Avg. Influence

2026

Latest

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01Top

#01

A controlled trial of leuprolide with and without flutamide in prostatic carcinoma.

HumanInfluence41.0

1440

The study demonstrated that combining leuprolide with flutamide significantly improves progression-free survival and median survival in men with advanced prostate cancer compared to leuprolide alone.

160 mgdaily(human)not mentioned120 mgorally(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly1 mgsubcutaneous(human)4 days200 µg/kgsubcutaneous(mouse)not mentioned300 µg/kgsubcutaneous(mouse)not mentioned

PubMed

02Top

#02

Ulipristal acetate versus leuprolide acetate for uterine fibroids.

HumanInfluence30.0

571

The study demonstrated that both 5 mg and 10 mg doses of ulipristal acetate were noninferior to leuprolide acetate in controlling uterine bleeding, with significantly fewer hot flashes reported in the ulipristal groups.

160 mgoral(human)daily120 mgoral(human)once daily240 mgsubcutaneous(human)for 1 month200 µg/kgsubcutaneous(mouse)not specified300 µg/kgsubcutaneous(mouse)not specified7.5 mgevery 28 days(human)not specified3.6 mgevery 28 days(human)not specified

PubMed

03Top

#03

The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer.

HumanInfluence27.0

558

The study demonstrated that degarelix was noninferior to leuprolide in maintaining testosterone suppression over 12 months, with faster testosterone and PSA suppression observed in the degarelix group.

PubMed

#04

Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer.

Shore Neal D, et al. · The New England journal of medicine · 2020

HumanInfluence33.0

323

The study demonstrated that relugolix achieved superior sustained testosterone suppression compared to leuprolide in men with advanced prostate cancer, with a significantly lower risk of major adverse cardiovascular events.

Key findings

0196.7% of men taking relugolix maintained low testosterone levels after 48 weeks, compared to 88.8% of those on leuprolide.
02Relugolix showed a significant advantage in achieving low testosterone levels quickly, with 56% of patients reaching these levels by day 4, while none on leuprolide did.
03The risk of major cardiovascular events was 54% lower in the relugolix group compared to the leuprolide group.

PubMed

#05

Efficacy and safety of ganirelix acetate versus leuprolide acetate in women undergoing controlled ovarian hyperstimulation.

HumanInfluence12.0

227

The study demonstrated that ganirelix acetate had similar pregnancy rates to leuprolide acetate but with fewer injection site reactions and a shorter treatment duration in women undergoing controlled ovarian hyperstimulation.

PubMed

#06

Improved Outcomes with Enzalutamide in Biochemically Recurrent Prostate Cancer.

Freedland Stephen J, et al. · The New England journal of medicine · 2023

HumanInfluence14.0

200

The study demonstrated that enzalutamide plus leuprolide significantly improved metastasis-free survival compared to leuprolide alone in patients with high-risk biochemical recurrence of prostate cancer.

Key findings

01Enzalutamide combined with androgen-deprivation therapy resulted in an 87.3% metastasis-free survival rate at 5 years, compared to 71.4% for androgen-deprivation therapy alone.
02Enzalutamide monotherapy also showed improved outcomes, with an 80.0% metastasis-free survival rate compared to leuprolide alone.
03The study found no new safety concerns and no significant differences in quality of life among the treatment groups.

PubMed

#07

Leuprolide acetate: a drug of diverse clinical applications.

ReviewInfluence3.0

187

Researchers observed that leuprolide acetate is a versatile GnRH agonist with potential applications across various clinical conditions beyond its established uses.

PubMed

#08

Clinical pharmacokinetics of depot leuprorelin.

Periti Piero, et al. · Clinical pharmacokinetics · 2002

ReviewInfluence6.0

154

Researchers studied leuprorelin acetate, a medication that reduces hormone production by using a special delivery method to avoid daily injections. They found that depot formulations can release the drug steadily over one to four months, maintaining effective levels in the body while being generally well tolerated.

Key findings

01Depot formulations of leuprorelin provide sustained drug release, reducing the need for frequent injections.
02Researchers observed that the drug maintains steady plasma concentrations for extended periods, depending on the formulation used.
03Local reactions at the injection site were more common with longer-acting depot versions compared to shorter ones.

PubMed

#09

The gonadotropin connection in Alzheimer's disease.

AnimalInfluence4.0

The study demonstrated that leuprolide acetate reduced amyloid-beta deposition and improved cognitive performance in aged transgenic mice, indicating a potential link between LH dysregulation and neurodegeneration in Alzheimer's disease.

PubMed

#10

New approaches to the therapy of various tumors based on peptide analogues.

ReviewInfluence4.0

The review highlighted that LH-RH agonists like leuprolide are preferred for treating advanced prostate cancer due to their efficacy in inhibiting pituitary and gonadal function.

160 mgdaily(human)not mentioned120 mgorally(human)not mentioned240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly300 µg/kgsubcutaneous(mouse)not mentioned

PubMed

Safety

Safety & Handling

Research Gaps

The long-term effects of leuprolide in combination with newer therapies like enzalutamide and relugolix remain unclear, particularly regarding overall survival beyond the 8-year mark and potential late-onset adverse effects. Additionally, the specific mechanisms by which leuprolide influences the efficacy of these newer agents in prostate cancer treatment have not been fully elucidated, leaving a gap in understanding the pharmacodynamic interactions between these therapies.

Solubility

Leuprolide is soluble in water and DMSO but has limited solubility in organic solvents like acetonitrile.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

🇩🇪DE

Approved as a medicinal product. Not a controlled substance.

🇺🇸US

Approved by the FDA for specific medical uses. Not a controlled substance.

🇦🇺AU

Approved by the TGA for specific medical uses.

🇬🇧UK

Approved by the MHRA for specific medical uses.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Publications per Year

48 total

Pricing

Price Comparison

BESTUmbrella LabsUS
10mg
$89.99
Price/mg
$9.00/mg
View
PeptaNovaEU
25mg
$226.80
Price/mg
$9.07/mg
View
Simple PeptideUS
6mg
$239.00
Price/mg
$39.83/mg
View
Alpha OmegaUS
6mg
$239.00
Price/mg
$39.83/mg
View
Umbrella LabsUS
100mg
—
Price/mg
—
View

Vendor	Amount	Price	Price/mg	Link
BESTUmbrella LabsUS	10mg	$89.99	$9.00/mg	View
PeptaNovaEU	25mg	$226.80	$9.07/mg	View
Simple PeptideUS	6mg	$239.00	$39.83/mg	View
Alpha OmegaUS	6mg	$239.00	$39.83/mg	View
Umbrella LabsUS	100mg	—	—	View

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Mechanism

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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer