Telotristat Ethyl

CHEMBL2105695 Phase 4 معتمد Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
575.0 g/mol
LogP
5.1
Phase
4

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.

الوزن الجزيئي

575,0000 g/mol

LogP

5,10

TPSA

131,00 Ų

قاعدة ليبينسكي للخمسة

راسب

المجالات العلاجية

Pharmacokinetics (PK)

Pharmacodynamics (PD)

البنية ثنائية الأبعاد

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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

الروابط القابلة للدوران

10

الذرات الثقيلة

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.

الأسئلة الشائعة

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 section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

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.

إخلاء المسؤولية الطبية

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.

Data sources: ChEMBL, PubChem, DailyMed.