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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 20:37:55 GMT 2025
Edited
by admin
on Mon Mar 31 20:37:55 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
9081Y98W2V
Record Status FAILED
Record Version
  • Download
Name Type Language
TRIPTORELIN
INN   MART.   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
ARVEKAP
Preferred 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
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 Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
NDF-RT N0000175655
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
LIVERTOX NBK548756
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
NCI_THESAURUS C242
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
WHO-VATC QL02AE04
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
NDF-RT N0000175654
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
WHO-ATC L02AE04
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
Code System Code Type Description
DRUG BANK
DB06825
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
PUBCHEM
25074470
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PRIMARY
CAS
57773-63-4
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PRIMARY
MERCK INDEX
m11194
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY Merck Index
CHEBI
63633
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
WIKIPEDIA
TRIPTORELIN
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
EPA CompTox
DTXSID2048375
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
SMS_ID
100000092206
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
ChEMBL
CHEMBL1201334
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
EVMPD
SUB11324MIG
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
INN
5711
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
DRUG CENTRAL
2968
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
DAILYMED
9081Y98W2V
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
USAN
W-59
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
NCI_THESAURUS
C1267
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
FDA UNII
9081Y98W2V
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
RXCUI
38782
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY RxNorm
IUPHAR
1177
Created by admin on Mon Mar 31 20:37:55 GMT 2025 , Edited by admin on Mon Mar 31 20:37:55 GMT 2025
PRIMARY
Related Record Type Details
TRIPTORELIN ACETATE
SALT/SOLVATE -> PARENT
GONADOTROPIN-RELEASING HORMONE RECEPTOR
TARGET -> AGONIST
TRIPTORELIN PAMOATE
INGREDIENT -> STARTING MATERIAL
TRIPTORELIN PAMOATE
SALT/SOLVATE -> PARENT
TRIPTORELIN ACETATE
INGREDIENT -> STARTING MATERIAL
Related Record Type Details
TRIPTORELIN
ACTIVE MOIETY

Structural Modifications

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