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Alpelisib

CHEMBL2396661 Phase 4 Disetujui Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
441.5 g/mol
LogP
3.2
Phase
4

A targeted cancer therapy that blocks PI3K-alpha, a specific enzyme that is often overactive due to PIK3CA gene mutations and drives the growth of certain breast, colorectal, and bladder cancers. By interrupting this signaling pathway, alpelisib can slow tumor growth, particularly in hormone receptor-positive, HER2-negative breast cancer.

Berat Molekul

441,5000 g/mol

LogP

3,20

TPSA

129,00 Ų

Lipinski RO5

Lulus

Area Terapeutik

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Non-Small Cell Lung Cancer Melanoma Non-Alcoholic Fatty Liver Disease Obesity Type 2 Diabetes Breast Cancer Prostate Cancer Colorectal Cancer

Mekanisme Kerja

Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mekanisme

Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

Struktur 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
Cc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1ccnc(C(C)(C)C(F)(F)F)c1

                

                

                
                

                    
InChI

                    
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C19H22F3N5O2S

                    

                    
                    

                        
HBD / HBA

                        
2 / 8

                    

                    
                    

                        
Ikatan yang Dapat Dirotasi

                        
4

                    

                    
                    
                    

                        
Atom Berat

                        
30

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Pertanyaan yang Sering Diajukan

                

                    
                    

                        
                        

                            
A targeted cancer therapy that blocks PI3K-alpha, a specific enzyme that is often overactive due to PIK3CA gene mutations and drives the growth of certain breast, colorectal, and bladder cancers. By interrupting this signaling pathway, alpelisib can slow tumor growth, particularly in hormone receptor-positive, HER2-negative breast cancer.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Alpelisib 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

    
    
        
        
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                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL2396661.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 56649450.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
Penyangkalan Medis

    

        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.