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Terfenadine

CHEMBL17157 Phase 4 承認済み Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
471.7 g/mol
LogP
6.6
Phase
4

Terfenadine was a first-generation selective peripheral histamine H1 receptor antagonist that was among the first non-sedating antihistamines, used for allergic rhinitis and urticaria. It was withdrawn from most markets due to its propensity to cause life-threatening QT prolongation and torsades de pointes arrhythmias, particularly when combined with CYP3A4 inhibitors or in patients with hepatic dysfunction, as the parent compound is cardiotoxic at higher plasma levels. Its active metabolite fexofenadine, which lacks cardiac toxicity, replaced terfenadine and remains in clinical use.

分子量

471.7000 g/mol

LogP

6.60

TPSA

43.70 Ų

リピンスキーの五則

適合

作用機序

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

機序

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

2D構造

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
CC(C)(C)c1ccc(C(O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3

                

                

                

                    
                    

                        
Molecular Formula

                        
C32H41NO2

                    

                    
                    

                        
HBD / HBA

                        
2 / 3

                    

                    
                    

                        
回転可能結合数

                        
9

                    

                    
                    
                    

                        
重原子数

                        
35

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
よくある質問

                

                    
                    

                        
                        

                            
Terfenadine was a first-generation selective peripheral histamine H1 receptor antagonist that was among the first non-sedating antihistamines, used for allergic rhinitis and urticaria. It was withdrawn from most markets due to its propensity to cause life-threatening QT prolongation and torsades de pointes arrhythmias, particularly when combined with CYP3A4 inhibitors or in patients with hepatic dysfunction, as the parent compound is cardiotoxic at higher plasma levels. Its active metabolite fexofenadine, which lacks cardiac toxicity, replaced terfenadine and remains in clinical use.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Terfenadine 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).
                CHEMBL17157.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 5405.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
医学的免責事項

    

        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.