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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.
Substance Class Protein
Created
by admin
on Mon Mar 31 20:47:55 GMT 2025
Edited
by admin
on Mon Mar 31 20:47:55 GMT 2025
Protein Sub Type
Record UNII
43OFW291R9
Record Status FAILED
Record Version
  • Download
Name Type Language
TRIPTORELIN ACETATE [MI]
Preferred Name English
TRIPTORELIN ACETATE
MART.   MI   WHO-DD  
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
Classification Tree Code System Code
NCI_THESAURUS C1910
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
Code System Code Type Description
MERCK INDEX
m11194
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY Merck Index
RXCUI
236538
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY RxNorm
RS_ITEM_NUM
1696131
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
FDA UNII
43OFW291R9
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
EVMPD
SUB04985MIG
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
PUBCHEM
25080282
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
NCI_THESAURUS
C128693
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
CAS
140194-24-7
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
DRUG BANK
DBSALT001171
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
SMS_ID
100000090505
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
DAILYMED
43OFW291R9
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
EPA CompTox
DTXSID301033427
Created by admin on Mon Mar 31 20:47:55 GMT 2025 , Edited by admin on Mon Mar 31 20:47:55 GMT 2025
PRIMARY
Related Record Type Details
TRIPTORELIN
PARENT -> SALT/SOLVATE
TRIPTORELIN
STARTING MATERIAL -> INGREDIENT
Related Record Type Details
TRIPTORELIN
ACTIVE MOIETY

Agent Modifications

Modification Process Modification Role Modification Type Amount Fragment Name Fragment ID
SALT FORMATION CHEMICAL Acetic acid Q40Q9N063P

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
MOIETY ACETATE ION 569DQM74SC
AMINO_ACID_SUBSTITUTION [1_1] N-TERMINUS PIDOLIC ACID SZB83O1W42
AMINO_ACID_SUBSTITUTION [1_10] C-TERMINUS GLYCINE GLYCINAMIDE 4JDT453NWO
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:SEQUENCE(CALCULATED) CHEMICAL
NIH
NCATS
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