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Leuprolide (Lupron)

Peptide

Leuprolide is a synthetic nonapeptide GnRH receptor agonist. FDA-approved since 1985, it is used for prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. Clinical trials show comparable efficacy to orchiectomy for prostate cancer and superior to placebo for endometriosis. Available as daily injection and depot formulations (1, 3, 4, and 6-month).

Quick Answer

What it is

Leuprolide is a synthetic nonapeptide GnRH receptor agonist. FDA-approved since 1985, it is used for prostate cancer, endometriosis, uterine fibroids, and central precocious puberty.

Key findings

  • Grade A: Testosterone Suppression (Prostate Cancer)
  • Grade A: PSA Reduction (Prostate Cancer)
  • Grade A: Disease Progression (Prostate Cancer)

Safety

No specific caution or interaction language was detected in the current summary/outcome notes.

⚠️ Research Notice

This peptide information is for educational and research purposes only. Peptides may not be FDA-approved for human use and may only be legally available for research purposes. Consult qualified healthcare professionals before considering any peptide compounds.

ℹ️ Quick Facts: Leuprolide (Lupron)

Quick Facts: Leuprolide (Lupron)

  • Best Evidence:Grade A
  • Conditions Studied:2
  • Research Outcomes:12
  • Grade A Findings:6
  • Grade B Findings:2
  • Key Effect:Prostate Cancer
A6
B2
C2
D2
2 conditions · 12 outcomes

Detailed Outcomes

|
A
Testosterone Suppression
Achieves castrate testosterone levels (<50 ng/dL) in 98%+ of patients. 6-month depot maintains suppression throughout treatment period.
large↓Improves
A
PSA Reduction
Significant PSA reduction in advanced prostate cancer. Comparable efficacy to bilateral orchiectomy in clinical trials.
large↓Improves
A
Disease Progression
Palliative treatment slows disease progression and improves quality of life in advanced prostate cancer.
large↓Improves
A
Pelvic Pain (Endometriosis)
Superior to placebo, comparable to danazol for pelvic pain reduction. Significant improvement in dysmenorrhea and dyspareunia.
large↓Improves
A
Endometriotic Lesions
Reduces size and number of endometriotic lesions. Objective improvement confirmed by laparoscopy in clinical trials.
large↓Improves
A
Dysmenorrhea
Significant reduction in menstrual pain. Comparable efficacy to intranasal buserelin 900 mcg/day.
large↓Improves
B
Anti-Cancer Activity
27 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
moderate↑Improves
B
Hormone Levels
8 human trials support this finding. Human clinical trial data available.
moderate↑Improves
C
Reproductive Outcomes
4 preclinical studies support this finding. Primarily preclinical evidence.
small↑Improves
D
Anti-Aging
2 human trials support this finding. Human clinical trial data available.
small↑Improves
D
Safety/Tolerability
2 human trials support this finding. Human clinical trial data available.
small↑Improves

Research Citations (43)

Leuprolide
(2023)
PMID: 31869126
Chronic periadolescent leuprolide exposure affects the development of reproductive physiology and behavior of female and male rats differently, but both mature after treatment termination.
(2023)
PMID: 36609535
Relugolix: A Review in Advanced Prostate Cancer.
(2023)
PMID: 36652173
Effects of Lupron and surgical castration on fecal androgen metabolite concentrations and intermale aggression in capybaras (Hydrochoerus hydrochaeris).
(2021)
PMID: 33338298
Patient preferences for elagolix and leuprolide for treating endometriosis-related pain in the United States.
(2021)
PMID: 33140977
Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide Acetate Treatment for Central Precocious Puberty.
(2020)
PMID: 32738042
Cost-effectiveness of elagolix versus leuprolide acetate for treating moderate-to-severe endometriosis pain in the USA.
(2019)
PMID: 30724096
Pharmacokinetic-Pharmacodynamic Model for the Testosterone-Suppressive Effect of Leuprolide in Normal and Prostate Cancer Rats.
(2018)
PMID: 29662027
Efficacy of Different Leuprolide Administration Schedules in Premenopausal Breast Cancer: A Retrospective Review.
(2018)
PMID: 29747931
Androgen deprivation therapy with Leuprolide acetate for treatment of advanced prostate cancer.
(2017)
PMID: 27826989

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