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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
157
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2470
 0.3 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8043
TRELSTAR

Approved Use

Indicated for the palliative treatment of advanced prostate cancer.

Launch Date

9.609408E11
PubMed

PubMed

TitleDatePubMed
Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics.
2000 Jul
Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
2001 Dec 7
GnRH analogues--agonists and antagonists.
2005 Aug
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.
Substance Class Protein
Created
by admin
on Fri Jun 25 23:00:52 UTC 2021
Edited
by admin
on Fri Jun 25 23:00:52 UTC 2021
Protein Sub Type
Record UNII
08AN7WA2G0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TRIPTORELIN PAMOATE
MI   ORANGE BOOK   USAN   VANDF  
USAN  
Official 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 EMBONATE
MART.   WHO-DD  
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 Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
FDA ORPHAN DRUG 34688
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
NCI_THESAURUS C1910
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C29523
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
MESH
D017329
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
MERCK INDEX
M11194
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY Merck Index
EPA CompTox
124508-66-3
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
PUBCHEM
25074469
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
ChEMBL
CHEMBL1201334
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
RXCUI
338529
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
RXCUI
905060
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
ALTERNATIVE
EVMPD
SUB16393MIG
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
CAS
1821299-86-8
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
ALTERNATIVE
FDA UNII
08AN7WA2G0
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
CAS
124508-66-3
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
DRUG BANK
DBSALT001256
Created by admin on Fri Jun 25 23:00:52 UTC 2021 , Edited by admin on Fri Jun 25 23:00:52 UTC 2021
PRIMARY
Related Record Type Details
TRIPTORELIN
PARENT -> SALT/SOLVATE
TRIPTORELIN
STARTING MATERIAL -> INGREDIENT
Related Record Type Details
TRIPTORELIN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
NIH
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