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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, primarily derived from the natural hormone GnRH. Researchers primarily study leuprolide for its role in androgen deprivation therapy, particularly in the management of prostate cancer. Key findings from recent studies indicate that leuprolide, when combined with enzalutamide, significantly improves metastasis-free survival compared to leuprolide alone, while also showing a slower testosterone suppression compared to newer agents like relugolix. Current research continues to explore its efficacy and safety in various treatment regimens, as well as its comparative effectiveness against emerging therapies.

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 anterior pituitary gland, leading to an initial surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. This surge eventually results in downregulation of GnRH receptors and decreased secretion of gonadotropins, thereby inhibiting the hypothalamic-pituitary-gonadal (HPG) axis and leading to reduced testosterone production in the testes. The precise molecular mechanisms underlying the long-term effects of leuprolide on signaling pathways involved in androgen receptor activity and prostate cancer progression are not fully understood.

Research

126 Research Publications

6,788

Total Citations

Human/RCT

4.3

Avg. Influence

2026

Latest

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01Top

#01

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

HumanInfluence41.0

1444

The study demonstrated that combining leuprolide with flutamide significantly improved progression-free survival and overall survival in patients with advanced prostate cancer compared to leuprolide alone.

120 mgoral(human)daily7.5 mgdepot(human)every 4 weeks200 µg/kgsubcutaneous(mouse)not mentioned300 µg/kgsubcutaneous(mouse)not mentioned

PubMed

02Top

#02

Ulipristal acetate versus leuprolide acetate for uterine fibroids.

HumanInfluence31.0

580

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

240 mgsubcutaneous(human)for 1 month160 mgdaily(human)daily

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

564

Researchers observed that degarelix maintained testosterone suppression effectively over 12 months and induced faster testosterone and PSA suppression compared to leuprolide in patients with prostate cancer.

240 mgsubcutaneous(human)for 1 month160 mgdaily(human)daily

PubMed

#04

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

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

HumanInfluence35.0

344

Researchers observed 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.

240 mgsubcutaneous(human)for 1 month160 mgdaily(human)daily

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 side effects and a higher one-year survival rate.

120 mgoral(human)daily7.5 mgdepot(human)every 4 weeks200 µg/kgsubcutaneous(mouse)not mentioned300 µg/kgsubcutaneous(mouse)not mentioned

PubMed

#06

Improved Outcomes with Enzalutamide in Biochemically Recurrent Prostate Cancer.

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

HumanInfluence18.0

240

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.

240 mgsubcutaneous(human)for 1 month160 mgdaily(human)daily

PubMed

#07

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

#08

Leuprolide acetate: a drug of diverse clinical applications.

ReviewInfluence3.0

195

Researchers observed that leuprolide acetate has diverse clinical applications, including potential roles in treating various conditions beyond reproductive health, such as Alzheimer's disease and functional bowel disease.

240 mgsubcutaneous(human)for 1 month160 mgdaily(human)daily

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

Polymer and microsphere blending to alter the release of a peptide from PLGA microspheres.

AnimalInfluence4.0

142

The study demonstrated that blending lower molecular weight PLGA polymers in microspheres enhanced the initial release of leuprolide acetate, leading to faster testosterone suppression in an animal model.

7.5 mgi.m.(human)every 28 days1 mgsc(human)4 days22.5 mgnot specified(human)not specified45 mgnot specified(human)not specified120 mgoral(human)not specified150 mg/daynot specified(human)not specified200 mg/twice-dailynot specified(human)not specified

PubMed

Safety

Safety & Handling

Research Gaps

The long-term effects of leuprolide in combination with newer agents like enzalutamide and relugolix on overall survival and quality of life remain unclear, as the final analysis of overall survival for enzalutide plus leuprolide has not been reported. Additionally, the specific mechanisms by which leuprolide interacts with these newer therapies and the potential for cumulative side effects over extended treatment periods are not well understood.

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

47 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
Behemoth LabzUS
45mg
—
Price/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
Behemoth LabzUS	45mg	—	—	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