Telotristat Ethyl
Telotristat ethyl is an oral tryptophan hydroxylase (TPH1) inhibitor that reduces serotonin synthesis in enterochromaffin cells, thereby decreasing urinary 5-HIAA levels and reducing the frequency and severity of diarrhea associated with carcinoid syndrome. It is approved as adjunctive therapy to somatostatin analogs in adults with carcinoid syndrome diarrhea not adequately controlled by somatostatin analog therapy. By targeting the peripheral enzyme TPH1 rather than the CNS enzyme TPH2, it reduces serotonin-mediated gut hypermotility without affecting central serotonin levels.
Molekularmasse
575,0000 g/mol
LogP
5,10
TPSA
131,00 Ų
Lipinski-Regel der Fünf
Nicht bestanden
Therapeutische Bereiche
Pharmacokinetics (PK)
Pharmacodynamics (PD)
2D-Struktur
Cite this structure
Embed this structure
SMILES
CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1
InChI
InChI=1S/C27H26ClF3N6O3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35)/t20-,24+/m0/s1
Molecular Formula
C27H26ClF3N6O3
HBD / HBA
2 / 11
Rotierbare Bindungen
10
Schwere Atome
40
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.
Häufig gestellte Fragen
Telotristat ethyl is an oral tryptophan hydroxylase (TPH1) inhibitor that reduces serotonin synthesis in enterochromaffin cells, thereby decreasing urinary 5-HIAA levels and reducing the frequency and severity of diarrhea associated with carcinoid syndrome. It is approved as adjunctive therapy to somatostatin analogs in adults with carcinoid syndrome diarrhea not adequately controlled by somatostatin analog therapy. By targeting the peripheral enzyme TPH1 rather than the CNS enzyme TPH2, it reduces serotonin-mediated gut hypermotility without affecting central serotonin levels.
Yes, Telotristat Ethyl is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL2105695. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 25181577. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
Medizinischer Haftungsausschluss
This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
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