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Trametinib

CHEMBL2103875 Phase 4 معتمد Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
615.4 g/mol
LogP
3.4
Phase
4

Trametinib is an oral allosteric MEK1/MEK2 inhibitor that blocks mitogen-activated protein kinase (MAPK) pathway signaling downstream of mutant BRAF and RAS oncoproteins, inhibiting tumor cell proliferation and promoting apoptosis in BRAF V600E/K-mutated cancers. It is approved in combination with dabrafenib for BRAF V600E/K-mutated melanoma, non-small cell lung cancer, anaplastic thyroid cancer, and solid tumors, and is under investigation for other RAS/MAPK-driven malignancies. The combination with BRAF inhibitors overcomes adaptive feedback reactivation of MEK that limits single-agent BRAF inhibitor efficacy.

الوزن الجزيئي

615,4000 g/mol

LogP

3,40

TPSA

102,00 Ų

قاعدة ليبينسكي للخمسة

ناجح

المجالات العلاجية

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

آلية العمل

Inhibits BRAF kinase, a key component of the RAS/MAPK signaling pathway, blocking constitutive activation that drives cancer cell proliferation in tumors harboring BRAF mutations.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

الآلية

Inhibits BRAF kinase, a key component of the RAS/MAPK signaling pathway, blocking constitutive activation that drives cancer cell proliferation in tumors harboring BRAF mutations.

البنية ثنائية الأبعاد

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
CC(=O)Nc1cccc(-n2c(=O)n(C3CC3)c(=O)c3c(Nc4ccc(I)cc4F)n(C)c(=O)c(C)c32)c1

                

                

                
                

                    
InChI

                    
InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)

                

                

                

                    
                    

                        
Molecular Formula

                        
C26H23FIN5O4

                    

                    
                    

                        
HBD / HBA

                        
2 / 6

                    

                    
                    

                        
الروابط القابلة للدوران

                        
5

                    

                    
                    
                    

                        
الذرات الثقيلة

                        
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.

    



                
            


            
            
            

                
الأسئلة الشائعة

                

                    
                    

                        
                        

                            
Trametinib is an oral allosteric MEK1/MEK2 inhibitor that blocks mitogen-activated protein kinase (MAPK) pathway signaling downstream of mutant BRAF and RAS oncoproteins, inhibiting tumor cell proliferation and promoting apoptosis in BRAF V600E/K-mutated cancers. It is approved in combination with dabrafenib for BRAF V600E/K-mutated melanoma, non-small cell lung cancer, anaplastic thyroid cancer, and solid tumors, and is under investigation for other RAS/MAPK-driven malignancies. The combination with BRAF inhibitors overcomes adaptive feedback reactivation of MEK that limits single-agent BRAF inhibitor efficacy.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Inhibits BRAF kinase, a key component of the RAS/MAPK signaling pathway, blocking constitutive activation that drives cancer cell proliferation in tumors harboring BRAF mutations.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Trametinib 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).
                CHEMBL2103875.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 11707110.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
إخلاء المسؤولية الطبية

    

        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.