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Gefapixant Citrate

CHEMBL4594278 Phase 4 Approved Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
545.5 g/mol
LogP
—
Phase
4

This citrate salt form of gefapixant is an oral P2X3 receptor antagonist used to reduce the frequency of chronic refractory cough by desensitizing the nerve pathways that trigger coughing. It offers a targeted, non-opioid approach to managing persistent cough that has not responded to other treatments.

Molecular Weight

545.5000 g/mol

TPSA

297.00 Ų

Mechanism of Action

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

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

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

2D Structure

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O.O=C(O)CC(O)(CC(=O)O)C(=O)O

                

                

                
                

                    
InChI

                    
InChI=1S/C14H19N5O4S.C6H8O7/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15;7-3(8)1-6(13,5(11)12)2-4(9)10/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)

                

                

                

                    
                    

                        
Molecular Formula

                        
C20H27N5O11S

                    

                    
                    

                        
HBD / HBA

                        
7 / 16

                    

                    
                    

                        
Rotatable Bonds

                        
10

                    

                    
                    
                    

                        
Heavy Atoms

                        
37

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Frequently Asked Questions

                

                    
                    

                        
                        

                            
This citrate salt form of gefapixant is an oral P2X3 receptor antagonist used to reduce the frequency of chronic refractory cough by desensitizing the nerve pathways that trigger coughing. It offers a targeted, non-opioid approach to managing persistent cough that has not responded to other treatments.

                        

                    

                    

                    

                    
                    

                        
                        

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

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Gefapixant Citrate 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).
                CHEMBL4594278.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 145720531.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
Medical Disclaimer

    

        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.