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Description
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

2000
172
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2752
 0.3 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8583
TRELSTAR

Approved Use

Indicated for the palliative treatment of advanced prostate cancer.

Launch Date

2000
PubMed

PubMed

TitleDatePubMed
GnRH analogues--agonists and antagonists.
2005-08
Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
2001-12-07
Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics.
2000-07
Patents

Patents

020715-001
3
021288-001
3

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 PAMOATE
MI   ORANGE BOOK   USAN   VANDF  
USAN  
Official Name English
TRIPTORELIN EMBONATE
MART.   WHO-DD  
Preferred Name English
TRIPTORELIN (AS EMBONATE)
Common Name English
TRELSTAR
Brand Name English
TRIPTORELIN PAMOATE [MI]
Common Name English
TRIPTORELIN PAMOATE [VANDF]
Common Name English
TRIPTORELIN PAMOATE [ORANGE BOOK]
Common Name English
SALVACYL
Brand Name English
5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYL-D-TRYPTOPHYL-L-LEUCYL-L-ARGINYL-L-PROLYLGLYCINE AMIDE, 4,4'-METHYLENEBIS(3-HYDROXY-2-NAPHTHOATE) (SALT)
Common Name English
LUTEINIZING HORMONE-RELEASING FACTOR (SWINE), 6-D-TRYPTOPHAN-, 4,4'-METHYLENEBIS(3-HYDROXY-2-NAPHTHALENECARBOXYLATE) (SALT)
Common Name English
DECAPEPTYL
Brand Name English
Triptorelin embonate [WHO-DD]
Common Name English
TRIPTORELIN EMBONATE [MART.]
Common Name English
TRIPTORELIN PAMOATE [USAN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 376012
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
FDA ORPHAN DRUG 34688
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
NCI_THESAURUS C1910
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C29523
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PRIMARY
MESH
D017329
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PRIMARY
MERCK INDEX
m11194
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PRIMARY Merck Index
SMS_ID
100000078575
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
EPA CompTox
DTXSID4046494
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
PUBCHEM
25074469
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
ChEMBL
CHEMBL1201334
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
USAN
MM-86
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
RXCUI
338529
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PRIMARY
RXCUI
905060
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ALTERNATIVE
EVMPD
SUB16393MIG
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PRIMARY
CAS
1821299-86-8
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
ALTERNATIVE
FDA UNII
08AN7WA2G0
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
CAS
124508-66-3
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
DAILYMED
08AN7WA2G0
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
DRUG BANK
DBSALT001256
Created by admin on Mon Mar 31 22:53:05 GMT 2025 , Edited by admin on Mon Mar 31 22:53:05 GMT 2025
PRIMARY
ACTIVE MOIETY
TRIPTORELIN
SUBSTANCE RECORD
TRIPTORELIN PAMOATE
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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