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GnRH agonist (triptorelin)
Triptorelin is a GnRH agonist that stimulates the pituitary gland to release luteinizing hormone and follicle-stimulating hormone, initially increasing sex hormone levels before causing desensitization and suppression of testosterone and estrogen production.
Triptorelin is a GnRH agonist that stimulates the pituitary gland to release luteinizing hormone and follicle-stimulating hormone, initially increasing sex hormone levels before causing desensitization and suppression of testosterone and estrogen production. Used for Advanced prostate cancer, Hormone-sensitive breast cancer, Precocious puberty.
At a glance
| Generic name | GnRH agonist (triptorelin) |
|---|---|
| Sponsor | Taipei Veterans General Hospital, Taiwan |
| Drug class | GnRH agonist |
| Target | GnRH receptor (GNRHR) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Triptorelin binds to GnRH receptors on pituitary gonadotroph cells, triggering an initial surge in LH and FSH release. With continuous exposure, the pituitary becomes desensitized, leading to downregulation of GnRH receptors and sustained suppression of gonadal sex hormone production. This mechanism is exploited therapeutically to reduce testosterone in prostate cancer and estrogen in hormone-sensitive breast cancer, or to suppress puberty progression in precocious puberty.
Approved indications
- Advanced prostate cancer
- Hormone-sensitive breast cancer
- Precocious puberty
- Endometriosis
Common side effects
- Hot flashes
- Erectile dysfunction
- Decreased libido
- Injection site reactions
- Headache
- Fatigue
- Gynecomastia
- Tumor flare (initial testosterone surge)
Key clinical trials
- Exploration of Treatment Effect of Novel Hormone Therapy Combined With Local Treatment Based on PSMA PET/CT Evaluation in mHSCP Patients (PHASE2)
- Refining Fertility-sparing Treatment in Endometrial Carcinoma Based on Molecular Classification (PHASE2, PHASE3)
- A Study of Adding Apalutamide to Radiotherapy and LHRH Agonist in High-Risk Patients With Hormone-Sensitive Prostate Cancer (PHASE3)
- Supraphysiologic Testosterone Priming Induces Darolutamide Extended Response (PHASE2)
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors (PHASE2)
- Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer (PHASE3)
- Hormone Therapy, Radiation Therapy, and Steroid 17alpha-monooxygenase TAK-700 in Treating Patients With High-Risk Prostate Cancer (PHASE3)
- Evaluating the Addition of Adjuvant Chemotherapy to Ovarian Function Suppression Plus Endocrine Therapy in Premenopausal Patients With pN0-1, ER-Positive/HER2-Negative Breast Cancer and an Oncotype Recurrence Score Less Than or Equal to 25 (PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |