Skip to content
Dr. Grey AI

Peptide

Leuprolide (Lupron)

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).

Research notice. This page is for education and research. Peptides may not be FDA-approved for human use and may only be legally available for research. Talk to a qualified clinician before considering any peptide.

Best evidence
Grade A
Conditions studied
2
Outcomes
11
Graded outcomes
6212

Evidence by condition

  • Strong
  • Moderate
  • Limited
  • Very limited

2 conditions, plus general outcomes

Prostate Cancer: outcomes studied for Leuprolide (Lupron)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Disease Progression

Palliative treatment slows disease progression and improves quality of life in advanced prostate cancer.

Improves (the measure goes down)Large effect17 studies
Testosterone Suppression

Achieves castrate testosterone levels (<50 ng/dL) in 98%+ of patients. 6-month depot maintains suppression throughout treatment period.

Improves (the measure goes down)Large effect15 studies

Studies that measured testosterone suppression

and 5 more in the citations list

PSA Reduction

Significant PSA reduction in advanced prostate cancer. Comparable efficacy to bilateral orchiectomy in clinical trials.

Improves (the measure goes down)Large effect15 studies
Endometriosis: outcomes studied for Leuprolide (Lupron)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Pelvic Pain (Endometriosis)

Superior to placebo, comparable to danazol for pelvic pain reduction. Significant improvement in dysmenorrhea and dyspareunia.

Improves (the measure goes down)Large effect16 studies
Endometriotic Lesions

Reduces size and number of endometriotic lesions. Objective improvement confirmed by laparoscopy in clinical trials.

Improves (the measure goes down)Large effect16 studies
Dysmenorrhea

Significant reduction in menstrual pain. Comparable efficacy to intranasal buserelin 900 mcg/day.

Improves (the measure goes down)Large effect16 studies

General

General: outcomes studied for Leuprolide (Lupron)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Anti-Cancer Activity

27 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Moderate effect15 studies

Studies that measured anti-cancer activity

and 5 more in the citations list

Hormone Levels

8 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Moderate effect11 studies

Studies that measured hormone levels

and 1 more in the citations list

Reproductive Outcomes

4 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect7 studies
Anti-Aging

2 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Small effect5 studies

Studies that measured anti-aging

Safety/Tolerability

2 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Small effect5 studies

Key findings

  • Disease ProgressionProstate CancerImproves (the measure goes down)
  • Pelvic Pain (Endometriosis)EndometriosisImproves (the measure goes down)
  • Endometriotic LesionsEndometriosisImproves (the measure goes down)

Studies cited

43 studies from PubMed

  1. LeuprolideStatPearls, 2023 · PMID 31869126
  2. Chronic periadolescent leuprolide exposure affects the development of reproductive physiology and behavior of female and male rats differently, but both mature after treatment termination.Biology of sex differences, 2023 · PMID 36609535
  3. Relugolix: A Review in Advanced Prostate Cancer.Targeted oncology, 2023 · PMID 36652173
  4. Effects of Lupron and surgical castration on fecal androgen metabolite concentrations and intermale aggression in capybaras (Hydrochoerus hydrochaeris).Zoo biology, 2021 · PMID 33338298
  5. Patient preferences for elagolix and leuprolide for treating endometriosis-related pain in the United States.Expert review of pharmacoeconomics & outcomes research, 2021 · PMID 33140977
  6. Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide Acetate Treatment for Central Precocious Puberty.The Journal of clinical endocrinology and metabolism, 2020 · PMID 32738042
  7. Cost-effectiveness of elagolix versus leuprolide acetate for treating moderate-to-severe endometriosis pain in the USA.Journal of comparative effectiveness research, 2019 · PMID 30724096
  8. Pharmacokinetic-Pharmacodynamic Model for the Testosterone-Suppressive Effect of Leuprolide in Normal and Prostate Cancer Rats.Molecules (Basel, Switzerland), 2018 · PMID 29662027
  9. Efficacy of Different Leuprolide Administration Schedules in Premenopausal Breast Cancer: A Retrospective Review.Clinical breast cancer, 2018 · PMID 29747931
  10. Androgen deprivation therapy with Leuprolide acetate for treatment of advanced prostate cancer.Expert opinion on pharmacotherapy, 2017 · PMID 27826989
  11. Extended release, 6-month formulations of leuprolide acetate for the treatment of advanced prostate cancer: achieving testosterone levels below 20 ng/dl.Expert opinion on drug metabolism & toxicology, 2015 · PMID 26293510
  12. Follicular mucinosis and mycosis-fungoides-like drug eruption due to leuprolide acetate: a case report and review.Journal of cutaneous pathology, 2012 · PMID 22882386
  13. GnRH agonists and antagonists in prostate cancerArch Ital Urol Androl, 2009 · PMID 19732971
  14. Leuprolide acetate: a drug of diverse clinical applicationsExpert Opin Investig Drugs, 2007 · PMID 17970643
  15. GnRH agonist Lupron (leuprolide acetate) pre-treatments prevent ovulation in response to gonadotropin stimulation in the clouded leopard (Neofelis nebulosa).Theriogenology, 2006 · PMID 16513161
  16. Leuprolide acetate given by a subcutaneous extended-release injection: less of a pain?Expert review of anticancer therapy, 2005 · PMID 16111462
  17. Leuprolide acetate 6-month depot formulation: safety and efficacy in advanced prostate cancerUrology, 2004 · PMID 16291585
  18. GnRH agonists in the treatment of endometriosis: the role of add-back therapyFertil Steril, 2001 · PMID 11704101
  19. Long-term survival and metastatic disease-free survival in patients with prostate cancer treated with leuprolide acetateUrology, 2001 · PMID 11684605
  20. Lupron depot prevention of antispermatogenic/antifertility activity of the indenopyridine, CDB-4022, in the rat.Biology of reproduction, 2001 · PMID 11420236
  21. Managing advanced prostate cancer with Viadur (leuprolide acetate implant).Urologic nursing, 2001 · PMID 11998504
  22. Chronic (60-week) toxicity study of DUROS leuprolide implants in dogs.International journal of toxicology, 2001 · PMID 11797819
  23. Leuprolide implant approved for once-yearly palliative treatment of advanced prostate cancer.Oncology (Williston Park, N.Y.), 2000 · PMID 10887633
  24. Effect of leuprolide acetate in treatment of abdominal pain and nausea in premenopausal women with functional bowel disease: a double-blind, placebo-controlled, randomized study.Digestive diseases and sciences, 1998 · PMID 9635630
  25. PSA levels and the rate of positive surgical margins in radical prostatectomy specimens preceded by androgen blockade in clinical B2 (T2bNxMo) prostate cancer. The Lupron Depot Neoadjuvant Study Group.Urology, 1997 · PMID 9123740
  26. Leuprolide in the treatment of endometrial cancer.Gynecologic oncology, 1997 · PMID 9299275
  27. Randomized prospective study comparing radical prostatectomy alone versus radical prostatectomy preceded by androgen blockade in clinical stage B2 (T2bNxM0) prostate cancer. The Lupron Depot Neoadjuvant Prostate Cancer Study Group.The Journal of urology, 1995 · PMID 7541859
  28. Unexpected pregnancies exposed to leuprolide acetate administered after the mid-luteal phase for ovarian stimulation.Human reproduction (Oxford, England), 1995 · PMID 7745056
  29. Leuprolide depot in the treatment of endometriosisClin Obstet Gynecol, 1993 · PMID 8164947
  30. Downstaging of localized prostate cancer by neoadjuvant therapy with flutamide and lupron: the first controlled and randomized trial.Clinical and investigative medicine. Medecine clinique et experimentale, 1993 · PMID 8013155
  31. Insulin resistance improves in hyperandrogenic women treated with Lupron.Fertility and sterility, 1993 · PMID 8405516
  32. Depot leuprolide acetate versus danazol in the treatment of women with symptomatic endometriosis: a multicenter, double-blind randomized clinical trial. II. Assessment of safety. The Lupron Endometriosis Study Group.American journal of obstetrics and gynecology, 1993 · PMID 8333471
  33. Nafarelin for endometriosis: a large-scale, danazol-controlled trial of efficacy and safety, with 1-year follow-up. The Nafarelin European Endometriosis Trial Group (NEET)Fertil Steril, 1992 · PMID 2140597
  34. Leuprolide with flutamide for complete androgen ablation: therapeutic alternative for advanced prostatic cancer (stage D2).Connecticut medicine, 1991 · PMID 1748007
  35. Lupron retards proliferation of ovarian epithelial tumor cells cultured in serum-free medium.The Journal of clinical endocrinology and metabolism, 1991 · PMID 1902482
  36. Drug induced polymyositis secondary to leuprolide acetate (Lupron) therapy for prostate carcinoma.Clinical and experimental rheumatology, 1991 · PMID 1954704
  37. Leuprorelin. A review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disordersDrugs, 1990 · PMID 7533699
  38. Leuprolide (TAP-144)--a general review.Journal of chemotherapy (Florence, Italy), 1989 · PMID 16312847
  39. Treatment of advanced prostatic cancer with leuprolide acetate depotUrology, 1988 · PMID 2898179
  40. Treatment of endometriosis with a long-acting gonadotropin-releasing hormone agonistFertil Steril, 1988 · PMID 3304710
  41. Leuprolide: a gonadotropin-releasing hormone analog for the palliative treatment of prostatic cancer.Drug intelligence & clinical pharmacy, 1986 · PMID 2429815
  42. Leuprolide versus diethylstilbestrol for metastatic prostate cancer. The Leuprolide Study GroupN Engl J Med, 1984 · PMID 3280182
  43. Leuprolide versus diethylstilbestrol for metastatic prostate cancer.The New England journal of medicine, 1984 · PMID 6436700