Triptorelin

Triptorelin (also known as Triptoreline, Triptorelina, Arvekap, Triptorelinum) is a anti-aging research peptide. Triptorelin is a gonadotropin-releasing hormone (GnRH) receptor agonist indicated for the treatment of advanced prostate cancer.

Triptorelin is a synthetic decapeptide and a gonadotropin-releasing hormone (GnRH) receptor agonist. It functions by initially stimulating and then desensitizing the GnRH receptors, leading to a reduction in gonadotropin secretion. Triptorelin is FDA-approved for the treatment of advanced prostate cancer and is also studied for conditions such as precocious puberty, endometriosis, and infertility. Research on triptorelin includes reviews on its use and associated adverse events, as well as clinical trials for central precocious puberty in children. It is marketed under the name Trelstar.

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
• Endometriosis
• Prostatic Neoplasms, Castration-Resistant
• Infertility
• Breast Neoplasms

2.2 Side effects

• Hot flushes
• Skeletal pain
• Impotence
• Headache
• Edema in legs
• Leg pain
• Erectile dysfunction
• Testicular atrophy

3 Chemical and physical properties

3.1 Amino acid sequence

4 Research dosages

3.75 mg every 4 weeks; 11.25 mg every 12 weeks; 22.5 mg every 24 weeks

5 Research studies (8)

1. Triptorelin
   (2012) · Review
2. Gonadotropin Releasing Hormone (GnRH) Analogues
   (2012) · Review
3. Triptorelin associated adverse events evaluated using FAERS pharmacovigilance data
   Scientific reports (2025)
4. Triptorelin for the treatment of endometriosis
   Expert opinion on pharmacotherapy (2014) · Review
5. A Phase 3, Open-Label, Single-Arm Trial of the Efficacy and Safety of Triptorelin 6-Month Formulation in Chinese Children with Central Precocious Puberty
   Advances in therapy (2024)
6. Triptorelin embonate (6-month formulation)
   Drugs (2010) · Review
7. An overview of treatments for endometriosis
   JAMA (2015) · Review
8. Triptorelin pamoate (Trelstar)
   The Medical letter on drugs and therapeutics (2002)

6 Safety and risk profile

6.1 Regulatory status

Triptorelin 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:

• Known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH

6.3 Drug interactions

6.4 Long-term risks

• anaphylactic shock, hypersensitivity, and angioedema
• worsening prostate cancer, spinal cord compression, and urinary tract obstruction
• metabolic changes such as hyperglycemia, diabetes, hyperlipidemia, and non-alcoholic fatty liver disease
• myocardial infarction, sudden cardiac death and stroke
• convulsions

6.5 Research best practices

• store at 20-25C (68-77F)
• do not freeze

7 Frequently asked questions

What is triptorelin used for?

Triptorelin is primarily used for the treatment of advanced prostate cancer. It is also investigated for other conditions such as precocious puberty, endometriosis, infertility, and castration-resistant prostatic neoplasms.

How does triptorelin work?

Triptorelin acts as a gonadotropin-releasing hormone (GnRH) receptor agonist. It initially stimulates GnRH receptors, leading to a transient increase in hormone levels, followed by desensitization of these receptors, which ultimately reduces the secretion of gonadotropins.

Is triptorelin FDA approved?

Yes, triptorelin is FDA approved. It received its first approval in the year 2000 and is indicated for the treatment of advanced prostate cancer.

What are the side effects of triptorelin?

Common side effects of triptorelin can include hot flushes, skeletal pain, impotence or erectile dysfunction, and headache. Other reported adverse reactions include edema in the legs, leg pain, and testicular atrophy.

What are the warnings associated with triptorelin?

Triptorelin carries warnings regarding hypersensitivity reactions, tumor flare (a transient worsening of prostate cancer symptoms), metabolic changes, increased risk of cardiovascular diseases, convulsions, severe cutaneous adverse reactions, and potential prolongation of the QT interval.

8 References

1. Triptorelin — compound summary PubChem. View source
2. Triptorelin — molecule record ChEMBL. View source
3. Triptorelin — FDA approved prescribing information U.S. Food and Drug Administration. View source
4. Triptorelin — published literature (1,001 records) PubMed. View source

9 See also

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