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Adagrasib

CHEMBL4594350 Phase 4 승인됨 Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
604.1 g/mol
LogP
5.0
Phase
4

Covalent trapping of a mutant oncoprotein defines adagrasib, which binds KRAS G12C selectively and irreversibly, locking the protein in its inactive GDP-bound state and shutting down downstream RAS/MAPK signalling. The cysteine introduced by the G12C substitution provides the anchor point, which is why activity is confined to tumours carrying that specific mutation and why molecular testing precedes treatment. Approved use covers adults with KRAS G12C-mutated non-small cell lung cancer and certain colorectal cancers that have progressed after previous therapy. KRAS had long been regarded as undruggable, and the covalent approach exploited by this class reversed that assessment. The compound is an orally administered small molecule, C32H35ClFN7O2, about 604.1 g/mol, approved and developed through the final clinical phase.

A targeted oral therapy designed to block a specific mutated protein called KRAS G12C, which drives uncontrolled cell growth in certain cancers when mutated. It is used in adults with KRAS G12C-mutated non-small cell lung cancer and certain colorectal cancers that have progressed after prior treatment. Patients' tumors must be tested for the specific KRAS G12C mutation before starting treatment to confirm likely benefit.

분자량

604.1000 g/mol

LogP

5.00

TPSA

88.80 Ų

리핀스키 5의 법칙

통과

치료 영역

Non-Small Cell Lung Cancer Oncology

작용 기전

Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

기전

Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream …

2D 구조

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N

                

                

                
                

                    
InChI

                    
InChI=1S/C32H35ClFN7O2/c1-21(34)31(42)41-17-16-40(18-23(41)11-13-35)30-25-12-15-39(28-10-4-7-22-6-3-9-26(33)29(22)28)19-27(25)36-32(37-30)43-20-24-8-5-14-38(24)2/h3-4,6-7,9-10,23-24H,1,5,8,11-12,14-20H2,2H3/t23-,24-/m0/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C32H35ClFN7O2

                    

                    
                    

                        
HBD / HBA

                        
- / 9

                    

                    
                    

                        
회전 가능 결합

                        
7

                    

                    
                    
                    

                        
무거운 원자

                        
43

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
자주 묻는 질문

                

                    
                    

                        
                        

                            
A targeted oral therapy designed to block a specific mutated protein called KRAS G12C, which drives uncontrolled cell growth in certain cancers when mutated. It is used in adults with KRAS G12C-mutated non-small cell lung cancer and certain colorectal cancers that have progressed after prior treatment. Patients' tumors must be tested for the specific KRAS G12C mutation before starting treatment to confirm likely benefit.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Adagrasib 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).
                CHEMBL4594350.
                Open-access bioactivity database.
            
        
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  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 138611145.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-08-20.




        


        
        
    


    



    
의학적 면책조항

    

        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.