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Leuprolide

Lupron · Leuprorelin · Eligard

Hormonal AxisApproved

MW: 1209.4g/mol
Formula: C59H84N16O12

Leuprolide is a synthetic peptide classified as a luteinizing hormone-releasing hormone (LHRH) agonist, primarily used in the management of hormone-sensitive conditions such as prostate cancer. Researchers primarily study leuprolide for its role in achieving androgen deprivation, which is critical in the treatment of advanced prostate cancer. Key findings from clinical trials indicate that leuprolide effectively suppresses testosterone levels, although it may initially cause a surge in testosterone before achieving its therapeutic effects. Studies also suggest that newer agents, such as relugolix, may offer more rapid and sustained testosterone suppression with a lower risk of adverse cardiovascular events compared to leuprolide. Current research continues to explore the efficacy and safety of leuprolide in combination therapies and its comparative effectiveness against emerging treatments.

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 an agonist at the GnRH receptors in the pituitary gland, leading to an initial surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. This surge subsequently results in downregulation of GnRH receptors, leading to decreased secretion of LH and FSH, which in turn reduces testosterone production in the testes via the steroidogenic signaling pathway. The overall biological process is androgen deprivation, which is critical in the management of hormone-sensitive prostate cancer.

Research

86 Research Publications

5,257

Total Citations

Human/RCT

6.0

Avg. Influence

2026

Latest

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01Top

#01

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

HumanInfluence41.0

1441

Researchers observed that leuprolide combined with flutamide resulted in longer progression-free survival and median survival in patients with advanced prostate cancer compared to leuprolide alone.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

02Top

#02

Ulipristal acetate versus leuprolide acetate for uterine fibroids.

HumanInfluence31.0

577

Researchers observed that ulipristal acetate was noninferior to leuprolide acetate in controlling uterine bleeding, with significantly fewer hot flashes reported in patients receiving ulipristal.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

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.

HumanInfluence28.0

560

Researchers observed that degarelix was noninferior to leuprolide in maintaining testosterone suppression over one year in human patients with prostate cancer, achieving faster testosterone and PSA suppression.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

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

327

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

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

#05

Leuprolide versus diethylstilbestrol for metastatic prostate cancer.

HumanInfluence1.0

250

Researchers observed that leuprolide and diethylstilbestrol had comparable efficacy in managing metastatic prostate cancer, but leuprolide was associated with fewer adverse effects and a higher one-year survival rate.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

#06

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

HumanInfluence12.0

226

Researchers observed that ganirelix acetate was effective and well tolerated, producing similar pregnancy rates compared to leuprolide acetate in women undergoing controlled ovarian hyperstimulation.

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

#07

Improved Outcomes with Enzalutamide in Biochemically Recurrent Prostate Cancer.

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

HumanInfluence14.0

206

Researchers observed that enzalutamide combined with leuprolide significantly improved metastasis-free survival compared to leuprolide alone in human 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.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

#08

Leuprolide acetate: a drug of diverse clinical applications.

ReviewInfluence3.0

189

Researchers observed that leuprolide acetate has diverse clinical applications, including potential roles in treating Alzheimer's disease, due to its mechanism of action on gonadotropin signaling.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

#09

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

#10

The gonadotropin connection in Alzheimer's disease.

AnimalInfluence4.0

Researchers observed that leuprolide acetate reduced amyloid generation and improved cognitive performance in aged transgenic mice, suggesting a potential link between gonadotropin signaling and neurodegeneration.

120 mgoral(human)48 weeks240 mgsubcutaneous(human)1 month80 mgsubcutaneous(human)monthly160 mgsubcutaneous(human)monthly200 µgsubcutaneous(mouse)not mentioned300 µgsubcutaneous(mouse)not mentioned

PubMed

Safety

Safety & Handling

Research Gaps

The long-term effects of leuprolide on overall survival and quality of life in patients with advanced prostate cancer remain unclear, as existing studies primarily focus on short-term outcomes. Additionally, the specific mechanisms by which leuprolide and other androgen-deprivation therapies influence cardiovascular risk and testosterone recovery post-treatment have not been fully elucidated in human trials.

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