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Difelikefalin

CHEMBL3989915 Phase 4 Approved Protein
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
679.8 g/mol
LogP
-0.6
Phase
4

A kappa opioid receptor agonist that reduces itch signals without crossing into the brain, used to treat moderate-to-severe chronic kidney disease-associated pruritus in dialysis patients. It works peripherally to relieve the intense itching common in this condition.

Molecular Weight

679.8000 g/mol

LogP

-0.60

TPSA

223.00 Ų

Lipinski RO5

Fail

Therapeutic Areas

Atopic Dermatitis Chronic Kidney Disease Rheumatoid Arthritis

Mechanism of Action

Binds to and activates its target receptor, mimicking the action of the endogenous ligand to produce a specific physiological response.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Binds to and activates its target receptor, mimicking the action of the endogenous ligand to produce a specific physiological response.

2D Structure

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
CC(C)C[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(C(=O)O)CC1

                

                

                
                

                    
InChI

                    
InChI=1S/C36H53N7O6/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49)/t27-,28-,29-,30-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C36H53N7O6

                    

                    
                    

                        
HBD / HBA

                        
7 / 9

                    

                    
                    

                        
Rotatable Bonds

                        
18

                    

                    
                    
                    

                        
Heavy Atoms

                        
49

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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

                

                    
                    

                        
                        

                            
A kappa opioid receptor agonist that reduces itch signals without crossing into the brain, used to treat moderate-to-severe chronic kidney disease-associated pruritus in dialysis patients. It works peripherally to relieve the intense itching common in this condition.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Binds to and activates its target receptor, mimicking the action of the endogenous ligand to produce a specific physiological response.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Difelikefalin is an approved drug. It has reached clinical phase 4. It is classified as a Protein.

                        

                    

                

            

            

            
            

            
            

            
            
{# 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).
                CHEMBL3989915.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 24794466.
                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.