Triptorelin

Summary

Triptorelin is a GnRH agonist used primarily for the treatment of advanced prostate cancer, endometriosis, uterine fibroids, and precocious puberty. It induces medical castration by suppressing sex hormone production through pituitary desensitization. Available in depot formulations for monthly, 3-month, or 6-month dosing intervals.

Mechanism of Action

Triptorelin is a synthetic analog of gonadotropin-releasing hormone (GnRH). Upon continuous administration, it causes desensitization and downregulation of pituitary GnRH receptors, leading to suppression of LH and FSH secretion, and consequently reducing gonadal steroid production (testosterone in males, estrogen in females) to castrate levels.

Routes of Administration

Goals & Uses

• Prostate cancer treatmentOncologyHigh
• Central precocious pubertyPediatric EndocrinologyHigh
• Uterine fibroid reductionGynecologyHigh
• Fertility preservation / controlled ovarian stimulationReproductive MedicineModerate
• Endometriosis managementGynecologyHigh
• Gender-affirming hormone therapyEndocrinologyModerate

Contraindications

• Spinal cord compression or urinary obstructionUrological/neurologicalHigh
• Undiagnosed vaginal bleedingGynecologicalModerate
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Hypersensitivity to GnRH, GnRH analogs, or triptorelinAllergyHigh
• BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data

Adverse Effects

• Injection site reactionsLocalCommon
• Decreased bone mineral densityMusculoskeletalCommon
• Erectile dysfunction / decreased libidoSexualCommon
• Hot flushes/flashesVasomotorCommon
• Testosterone flareEndocrineCommon
• Cardiovascular events (QT prolongation, metabolic syndrome)Cardiovascular/metabolicUncommon

Drug Interactions

• Antidiabetic agentsModerate
• Antiandrogens (e.g., bicalutamide)Low
• QT-prolonging agents (e.g., antiarrhythmics, antipsychotics)High
• Warfarin / anticoagulantsModerate

Population Constraints

• Elderly patients with cardiovascular diseaseCardiovascularRelative
• Pediatric patients (non-precocious puberty use)AgeRelative
• Patients with diabetes mellitusMetabolicRelative
• Patients with osteoporosisMusculoskeletalRelative

Regulatory Status

• European UnionApprovedApproved: Advanced prostate cancer, Endometriosis, Uterine fibroids, Central precocious pubertyApproved under brand names Decapeptyl and Gonapeptyl; broader indication set than US approval.
• United StatesApprovedApproved: Palliative treatment of advanced prostate cancerApproved by FDA under brand name Trelstar (Watson/Allergan). Available in 3.75 mg, 11.25 mg, and 22.5 mg depot formulations.
• United KingdomApprovedApproved: Prostate cancer, Endometriosis, Uterine fibroids, Central precocious pubertyApproved by MHRA; available under Decapeptyl brand. Used in NHS gender identity clinics for puberty suppression in adolescents under NHS England policy.

Approved by the FDA (Trelstar) for palliative treatment of advanced prostate cancer. Also approved in the EU under various brand names for prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. Classified as a prescription-only medicine across all jurisdictions.

Evidence & Sources

No sources recorded yet.