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.
Berat Molekul
575,0000 g/mol
LogP
5,10
TPSA
131,00 Ų
Lipinski RO5
Gagal
Area Terapeutik
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Struktur 2D
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
Ikatan yang Dapat Dirotasi
10
Atom Berat
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.
Pertanyaan yang Sering Diajukan
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.
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