TRIPTORELIN ACETATE

Description
Sources: http://www.drugbank.ca/drugs/DB06825
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020715s024,021288s021,022437s002lbl.pdf

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 Target ID: CHEMBL1855 Sources: http://www.drugbank.ca/drugs/DB06825	Agonist 2678		0.3 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Advanced prostate cancer 9 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020715s024,021288s021,022437s002lbl.pdf	Palliative		Approved 8429	TRELSTAR Approved Use Indicated for the palliative treatment of advanced prostate cancer. Launch Date 2000

PubMed

Title	Date	PubMed
Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.	2001 Dec 7	11726197
GnRH analogues--agonists and antagonists.	2005 Aug	15955640

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.

Name

Type

Language

TRIPTORELIN ACETATE

Common Name

English

TRIPTORELIN ACETATE [GREEN BOOK]

Common Name

English

TRIPTORELIN ACETATE [USP-RS]

Common Name

English

Triptorelin acetate [WHO-DD]

Common Name

English

TRIPTORELIN ACETATE [MART.]

Common Name

English

TRIPTORELIN ACETATE [MI]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1910