Leuprolide

Leuprolide (also known as Leuprorelin, Leuprorelina, Leuproreline, Leuprorelinum) is a anti-aging research peptide. Leuprolide is a gonadotropin-releasing hormone (GnRH) receptor agonist used in the treatment of advanced prostate cancer and other hormone-sensitive conditions.

Leuprolide, also known as leuprorelin, is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH). It functions as a GnRH receptor agonist, initially stimulating and then desensitizing the receptor, leading to a decrease in gonadotropin secretion and subsequent reduction in sex hormone levels. This mechanism makes it effective in treating hormone-dependent conditions. Leuprolide is FDA-approved for advanced prostate cancer and has been studied for conditions such as precocious puberty, endometriosis, and breast neoplasms. Research on leuprolide has explored its use in various cancers and hormone-related disorders, with over 2,300 papers mentioning it.

1 Mechanism of action

Gonadotropin-releasing hormone receptor agonist (agonist)

Primary targets: Gonadotropin-releasing hormone receptor

2 Reported effects

Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.

2.1 Indicated / studied for

• Advanced prostate cancer
• Prostatic Neoplasms
• Puberty, Precocious
• Leiomyoma
• Obesity
• Endometriosis
• Breast Neoplasms
• Infertility, Male
• Hodgkin Disease

2.2 Side effects

• Malaise
• Fatigue
• Hot flashes/sweats
• Testicular atrophy
• Decreased bone density
• Pituitary apoplexy

3 Chemical and physical properties

3.1 Amino acid sequence

4 Research dosages

7.5 mg subcutaneously every month; 22.5 mg subcutaneously every 3 months; 30 mg subcutaneously every 4 months; 45 mg subcutaneously every 6 months

5 Research studies (8)

1. Improved Outcomes with Enzalutamide in Biochemically Recurrent Prostate Cancer
   The New England journal of medicine (2023) · RCT
2. Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer
   The New England journal of medicine (2020) · RCT
3. Improved Survival with Enzalutamide in Biochemically Recurrent Prostate Cancer
   The New England journal of medicine (2026) · RCT
4. Leuprolide
   (2012) · Review
5. Leuprolide
   (2026)
6. The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer
   BJU international (2008) · RCT
7. Degarelix
   Drugs (2009)
8. Testosterone Recovery for Relugolix Versus Leuprolide in Men with Advanced Prostate Cancer: Results from the Phase 3 HERO Study
   European urology oncology (2024) · RCT

6 Safety and risk profile

6.1 Regulatory status

Leuprolide is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.

6.2 Contraindications

Conditions and populations in which use is contraindicated:

• Hypersensitivity to GnRH
• Hypersensitivity to GnRH agonist analogs
• Hypersensitivity to any components of VABRINTY

6.3 Long-term risks

• Tumor Flare (worsening of symptoms or onset of new signs and symptoms, including bone pain, neuropathy, hematuria, bladder outlet obstruction, ureteral obstruction, or spinal cord compression)
• Hyperglycemia and diabetes
• Cardiovascular diseases (myocardial infarction, sudden cardiac death and stroke)
• QT/QTc Interval prolongation
• Convulsions
• Severe Cutaneous Adverse Reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis
• Embryo-Fetal Toxicity

6.4 Research best practices

• Store at 2°C to 8°C (36°F to 46°F)
• May be stored in original packaging at room temperature 15°C to 30°C (59°F to 86°F) for up to eight weeks prior to mixing and administration

7 Frequently asked questions

What is leuprolide used for?

Leuprolide is primarily indicated for the treatment of advanced prostate cancer. It is also studied and used for other hormone-sensitive conditions such as precocious puberty, endometriosis, leiomyoma, and breast neoplasms due to its effect on sex hormone levels.

How does leuprolide work?

Leuprolide works as a gonadotropin-releasing hormone (GnRH) receptor agonist. Initially, it stimulates the GnRH receptor, leading to a transient increase in sex hormones. However, with continuous administration, it desensitizes the receptor, which ultimately suppresses the release of gonadotropins and reduces the production of sex hormones like testosterone and estrogen.

Is leuprolide FDA approved?

Yes, leuprolide is FDA approved. It received its first approval in 1985 and is marketed under brand names such as Vabrinty for the treatment of advanced prostate cancer.

What are the side effects of leuprolide?

Common side effects of leuprolide include malaise, fatigue, hot flashes/sweats, and testicular atrophy. Other reported adverse reactions include decreased bone density and rare cases of pituitary apoplexy. Patients should be monitored for potential tumor flare, hyperglycemia, cardiovascular issues, and severe cutaneous adverse reactions.

What warnings are associated with leuprolide?

Leuprolide carries warnings regarding tumor flare, which can worsen symptoms during the initial weeks of treatment. Other serious warnings include hyperglycemia and an increased risk of developing diabetes, cardiovascular diseases like myocardial infarction and stroke, QT/QTc interval prolongation, convulsions, and severe cutaneous adverse reactions. It may also cause fetal harm.

8 References

1. Leuprolide — compound summary PubChem. View source
2. Leuprolide — molecule record ChEMBL. View source
3. Leuprolide — FDA approved prescribing information U.S. Food and Drug Administration. View source
4. Leuprolide — published literature (2,349 records) PubMed. View source

9 See also

• Peptide encyclopedia index
• Peptide reconstitution calculator
• Glossary of peptide research terms