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Triptorelin (GnRH agonists)
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 sustained suppression through receptor desensitization.
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 sustained suppression through receptor desensitization. Used for Advanced prostate cancer, Breast cancer (premenopausal women), Endometriosis.
At a glance
| Generic name | Triptorelin (GnRH agonists) |
|---|---|
| Sponsor | University of Pisa |
| Drug class | GnRH agonist |
| Target | GnRH receptor (GNRHR) |
| Modality | Small molecule |
| Therapeutic area | Oncology, Endocrinology |
| Phase | FDA-approved |
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 and downregulates GnRH receptors, resulting in profound suppression of testosterone and estrogen production. This sustained hormonal suppression is therapeutically exploited in hormone-dependent cancers and certain reproductive disorders.
Approved indications
- Advanced prostate cancer
- Breast cancer (premenopausal women)
- Endometriosis
- Uterine fibroids
- Central precocious puberty
Common side effects
- Hot flashes
- Erectile dysfunction
- Decreased libido
- Injection site reactions
- Headache
- Gynecomastia
- Bone density loss (with prolonged use)
Key clinical trials
- Radiotherapy After Prostatectomy for Node Positive Prostate Cancer (PHASE3)
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors (PHASE2)
- Hormone Therapy, Radiation Therapy, and Steroid 17alpha-monooxygenase TAK-700 in Treating Patients With High-Risk Prostate Cancer (PHASE3)
- Pembrolizumab With Androgen Deprivation Therapy and Radiotherapy for the Treatment of Patients With High Risk Localized Prostate Cancer (PHASE2)
- ODM-201 vs Androgen Deprivation Therapy in Hormone naïve Prostate Cancer (PHASE2)
- Management of Castration-Resistant Prostate Cancer with Oligometastases (PHASE2, PHASE3)
- Triptorelin for Early Diagnosis of Hypogonadotrophic Hypogonadism (NA)
- Radiotherapy Combined With a LHRH (Ant)Agonist Versus Apalutamide in Patients With Biochemical Recurrence After RP (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |