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Telotristat Ethyl

CHEMBL2105695 Phase 4 Đã phê duyệt 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.

Khối lượng phân tử

575,0000 g/mol

LogP

5,10

TPSA

131,00 Ų

Lipinski RO5

Không đạt

Lĩnh vực điều trị

Pancreatic Cancer

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Cấu trúc 2D

SVG PNG

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

                    

                    
                    

                        
Liên kết có thể quay

                        
10

                    

                    
                    
                    

                        
Nguyên tử nặng

                        
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.

    



                
            


            
            
            

                
Câu hỏi thường gặp

                

                    
                    

                        
                        

                            
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.




        


        
        
    


    



    
Tuyên bố miễn trách y tế

    

        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.