U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
171
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
 0.3 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8429
TRELSTAR

Approved Use

Indicated for the palliative treatment of advanced prostate cancer.

Launch Date

2000
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.
Name Type Language
TRIPTORELIN
INN   MART.   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
TRIPTORELIN [MI]
Common Name English
CL 118,532
Code English
TRIPTORELIN [MART.]
Common Name English
5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYL-D-TRYPTOPHYL-L-LEUCYL-L-ARGINYL-L-PROLYLGLYCINAMIDE
Common Name English
TRIPTORELIN [USAN]
Common Name English
TRIPTODUR
Brand Name English
WY-42462
Code English
CL-118532
Code English
triptorelin [INN]
Common Name English
ARVEKAP
Brand Name English
AY-25650
Code English
TRIPTORELIN [VANDF]
Common Name English
TRYPTORELIN
Common Name English
Triptorelin [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C1910
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
NDF-RT N0000175655
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
LIVERTOX NBK548756
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
NCI_THESAURUS C242
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
WHO-VATC QL02AE04
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
NDF-RT N0000175654
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
WHO-ATC L02AE04
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
Code System Code Type Description
DRUG BANK
DB06825
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
PUBCHEM
25074470
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
CAS
57773-63-4
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
MERCK INDEX
m11194
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY Merck Index
CHEBI
63633
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
WIKIPEDIA
TRIPTORELIN
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
EPA CompTox
DTXSID2048375
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
SMS_ID
100000092206
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
ChEMBL
CHEMBL1201334
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
EVMPD
SUB11324MIG
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
INN
5711
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
DRUG CENTRAL
2968
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
DAILYMED
9081Y98W2V
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
USAN
W-59
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
NCI_THESAURUS
C1267
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
FDA UNII
9081Y98W2V
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
RXCUI
38782
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY RxNorm
IUPHAR
1177
Created by admin on Sat Dec 16 00:36:38 GMT 2023 , Edited by admin on Sat Dec 16 00:36:38 GMT 2023
PRIMARY
ACTIVE MOIETY
TRIPTORELIN
SALT/SOLVATE (PARENT)
TRIPTORELIN ACETATE
SALT/SOLVATE (PARENT)
TRIPTORELIN PAMOATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966