TRIPTORELIN

Description

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). It works by decreasing the production of certain hormones, which reduces testosterone levels in the body. Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone. Triptorelin is indicated for the palliative treatment of advanced prostate cancer.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Gonadotropin-releasing hormone receptor 41	Agonist 2,678		0.3 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Advanced prostate cancer 9	Palliative		Approved 8,429	TRELSTAR

PubMed

Show entries

Title	Date	PubMed
Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.	2001 Dec 7	11726197

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Patents

Sample Use Guides

In Vivo Use Guide

Administered as a single intramuscular injection in either buttock. Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule. • 3.75 mg every 4 weeks. • 11.25 mg every 12 weeks • 22.5 mg every 24 weeks

Route of Administration: Intramuscular

In Vitro Use Guide

Triptorelin stimulates both oxytocin (OT) and vasopressin (AVP) release from the rat hypothalamo-neurohypophysial (H-N) system at concentrations of 10(-9)-10(-5) M. The strongest effect was displayed by triptorelin at a concentration of 10(-7) M.