Triptorelin
Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) that, upon continuous administration, causes pituitary desensitization and downregulation of GnRH receptors, leading to suppression of luteinizing hormone, follicle-stimulating hormone, and consequently sex hormone production. It is used for prostate cancer (androgen deprivation therapy), breast cancer, endometriosis, and precocious puberty. Its mechanism exploits the paradox that continuous GnRH receptor stimulation leads to receptor desensitization and hormonal castration.
Masse moléculaire
1311,4000 g/mol
LogP
-0,30
TPSA
490,00 Ų
Règle des 5 de Lipinski
Non conforme
Aires thérapeutiques
Mécanisme d'action
Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.
Structure 2D
Cite this structure
Embed this structure
SMILES
CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O
InChI
InChI=1S/C64H82N18O13/c1-34(2)23-46(56(88)75-45(13-7-21-69-64(66)67)63(95)82-22-8-14-52(82)62(94)72-31-53(65)85)76-58(90)48(25-36-28-70-42-11-5-3-9-40(36)42)78-57(89)47(24-35-15-17-39(84)18-16-35)77-61(93)51(32-83)81-59(91)49(26-37-29-71-43-12-6-4-10-41(37)43)79-60(92)50(27-38-30-68-33-73-38)80-55(87)44-19-20-54(86)74-44/h3-6,9-12,15-18,28-30,33-34,44-52,70-71,83-84H,7-8,13-14,19-27,31-32H2,1-2H3,(H2,65,85)(H,68,73)(H,72,94)(H,74,86)(H,75,88)(H,76,90)(H,77,93)(H,78,89)(H,79,92)(H,80,87)(H,81,91)(H4,66,67,69)/t44-,45-,46-,47-,48+,49-,50-,51-,52-/m0/s1
Molecular Formula
C64H82N18O13
HBD / HBA
17 / 15
Liaisons Rotatives
33
Atomes Lourds
95
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Foire aux questions
Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) that, upon continuous administration, causes pituitary desensitization and downregulation of GnRH receptors, leading to suppression of luteinizing hormone, follicle-stimulating hormone, and consequently sex hormone production. It is used for prostate cancer (androgen deprivation therapy), breast cancer, endometriosis, and precocious puberty. Its mechanism exploits the paradox that continuous GnRH receptor stimulation leads to receptor desensitization and hormonal castration.
Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.
Yes, Triptorelin is an approved drug. It has reached clinical phase 4. It is classified as a Protein.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1201334. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 25074470. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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