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Osimertinib

CHEMBL3353410 Phase 4 Approved Small molecule
Half-Life
48 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
499.6 g/mol
LogP
3.7
Phase
4

A third-generation EGFR inhibitor targeting specific mutations including T790M resistance in lung cancer.

Molecular Weight

499.6050 g/mol

LogP

3.70

TPSA

87.60 Ų

Lipinski RO5

Pass

Therapeutic Areas

Bladder Cancer Breast Cancer Colorectal Cancer Lymphoma Melanoma Non-Small Cell Lung Cancer Oncology Ovarian Cancer Pancreatic Cancer Prostate Cancer Thyroid Cancer

Drug Classes

L — L - Antineoplastic and Immunomodulating Agents

Mechanism of Action

Third-generation irreversible EGFR TKI targeting T790M resistance mutation and activating mutations.

Pharmacokinetics (PK)

Half-Life 48 hours

Pharmacodynamics (PD)

Mechanism

Third-generation irreversible EGFR TKI targeting T790M resistance mutation and activating mutations.

2D Structure

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C

                

                

                
                

                    
InChI

                    
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)

                

                

                

                    
                    

                        
Molecular Formula

                        
C28H33N7O2

                    

                    
                    

                        
HBD / HBA

                        
2 / 7

                    

                    
                    

                        
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

                

                    
                    

                        
                        

                            
A third-generation EGFR inhibitor targeting specific mutations including T790M resistance in lung cancer.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Third-generation irreversible EGFR TKI targeting T790M resistance mutation and activating mutations.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Osimertinib: Half-life: 48 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Osimertinib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            
            

                
                
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{# 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).
                CHEMBL3353410.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 71496458.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
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.