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Tucatinib

CHEMBL3989868 Phase 4 已批准 Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
480.5 g/mol
LogP
4.0
Phase
4

This oral targeted therapy is a HER2-specific tyrosine kinase inhibitor used in combination with trastuzumab and capecitabine to treat HER2-positive breast cancer that has spread to the brain or other parts of the body, particularly after prior HER2-based therapy. It is notable for its ability to penetrate the blood-brain barrier, making it effective against brain metastases. Diarrhea and liver enzyme elevations are common side effects that require monitoring.

分子量

480.5000 g/mol

LogP

4.00

TPSA

111.00 Ų

Lipinski 五规则

符合

治疗领域

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Endometriosis Benign Prostatic Hyperplasia Glaucoma Cardiovascular Disease Age-Related Macular Degeneration Neurology Psychiatry Endocrinology Respiratory Disease Dermatology Hematology Pain Management Ophthalmology Non-Small Cell Lung Cancer Rheumatoid Arthritis Osteoporosis Asthma Chronic Obstructive Pulmonary Disease Immunology Alzheimer's Disease Parkinson's Disease Epilepsy Migraine Schizophrenia Bipolar Disorder Generalized Anxiety Disorder Insomnia Infectious Disease Melanoma Hepatology Oncology Nephrology Gastroesophageal Reflux Disease Inflammatory Bowel Disease Psoriasis Obstetrics & Gynecology Anesthesiology Systemic Lupus Erythematosus Multiple Sclerosis Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Urology Stroke Deep Vein Thrombosis / Pulmonary Embolism Hyperlipidemia Obesity Lymphoma Gastroenterology Rheumatology Transplant Medicine Type 2 Diabetes Hypertension Major Depressive Disorder Breast Cancer Atopic Dermatitis Gout Chronic Pain Malaria HIV/AIDS Hepatitis C Tuberculosis Heart Failure Atrial Fibrillation Prostate Cancer Colorectal Cancer Leukemia

作用机制

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

Pharmacokinetics (PK)

Pharmacodynamics (PD)

机制

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

二维结构

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1

                

                

                
                

                    
InChI

                    
InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31)

                

                

                

                    
                    

                        
Molecular Formula

                        
C26H24N8O2

                    

                    
                    

                        
HBD / HBA

                        
2 / 8

                    

                    
                    

                        
可旋转键数

                        
6

                    

                    
                    
                    

                        
重原子数

                        
36

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
常见问题

                

                    
                    

                        
                        

                            
This oral targeted therapy is a HER2-specific tyrosine kinase inhibitor used in combination with trastuzumab and capecitabine to treat HER2-positive breast cancer that has spread to the brain or other parts of the body, particularly after prior HER2-based therapy. It is notable for its ability to penetrate the blood-brain barrier, making it effective against brain metastases. Diarrhea and liver enzyme elevations are common side effects that require monitoring.

                        

                    

                    

                    

                    
                    

                        
                        

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

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Tucatinib 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

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL3989868.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 51039094.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
医疗免责声明

    

        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.