OncologyFDA Approved

Triptorelin (Trelstar)

Intramuscular injection

Overview

Triptorelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) that functions as a long-acting GnRH agonist. Following an initial stimulatory phase, chronic administration leads to downregulation of pituitary GnRH receptors, resulting in suppression of luteinizing hormone and follicle-stimulating hormone secretion and subsequent reduction in sex steroid production.

Mechanism of Action

This mechanism provides therapeutic benefit in hormone-sensitive conditions including advanced prostate cancer, endometriosis, and central precocious puberty. The peptide incorporates amino acid substitutions at positions 6 and 10 to enhance receptor affinity and metabolic stability..

Research Summary & Key Findings

Triptorelin received FDA approval in 2000 for palliative treatment of advanced prostate cancer, with pivotal trials demonstrating effective castration in over 90% of patients maintained on depot formulations. Comparative studies have shown equivalent efficacy to other GnRH agonists such as leuprolide and goserelin in achieving and maintaining testosterone suppression. Long-term extension studies have confirmed durability of response with acceptable tolerability profiles across approved depot formulations (1-month, 3-month, and 6-month).

Clinical Status

FDA Approved

Triptorelin (Trelstar) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Administration Routes

Intramuscular injection

Related Peptides in Oncology

Carfilzomib (Kyprolis)

FDA Approved

A tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds the chymotrypsin-like (beta5) subunit of the 20S...

View details

Bortezomib (Velcade)

FDA Approved

A modified dipeptidyl boronic acid that reversibly inhibits the chymotrypsin-like activity of the 26S proteasome. Bortez...

View details

Lutetium-177 dotatate (Lutathera)

FDA Approved

A radiolabeled somatostatin analog consisting of the peptide DOTA-Tyr3-octreotate chelated to the beta-emitting radioiso...

View details

Leuprolide (Lupron) - Oncology

FDA Approved

A GnRH agonist used in oncology for androgen deprivation therapy (ADT) in prostate cancer and hormone suppression in pre...

View details

Find a Provider

Find a verified provider who offers Triptorelin (Trelstar) therapy in your area.

Browse Provider Map

Find a Pharmacy

Browse PCAB-accredited and FDA 503B-registered compounding pharmacies that supply Triptorelin (Trelstar).

Pharmacy Directory

Join the Association

Access exclusive peptide protocols, provider resources, and community support.

List Your Practice

Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol.