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Tamoxifen

CHEMBL83 Phase 4 Approved Small molecule
Half-Life
5-7 days
Bioavailability
—
Protein Binding
—
Molecular Weight
371.5 g/mol
LogP
7.1
Phase
4

This medication blocks estrogen receptors in breast tissue and is widely used to treat and reduce the risk of hormone receptor-positive breast cancer in both women and men. It is typically taken as a daily tablet for five to ten years as part of a long-term cancer prevention or treatment plan. Regular gynecologic check-ups are recommended because it can have estrogen-like effects on the uterus.

Molecular Weight

371.5150 g/mol

LogP

7.10

TPSA

12.50 Ų

Lipinski RO5

Pass

Therapeutic Areas

Alzheimer's Disease Benign Prostatic Hyperplasia Bipolar Disorder Bladder Cancer Breast Cancer Cardiovascular Disease Chronic Kidney Disease Chronic Obstructive Pulmonary Disease Chronic Pain Colorectal Cancer Endometriosis Gastroesophageal Reflux Disease Hepatitis C HIV/AIDS Hypertension Infectious Disease Inflammatory Bowel Disease Lymphoma Melanoma Non-Alcoholic Fatty Liver Disease Non-Small Cell Lung Cancer Obesity Osteoporosis Ovarian Cancer Pain Management Pancreatic Cancer Parkinson's Disease Prostate Cancer Respiratory Disease Rheumatoid Arthritis Schizophrenia Thyroid Cancer

Drug Classes

L — L - Antineoplastic and Immunomodulating Agents

Mechanism of Action

Selective estrogen receptor modulator (SERM).

Pharmacokinetics (PK)

Half-Life 5-7 days

Pharmacodynamics (PD)

Mechanism

Selective estrogen receptor modulator (SERM).

2D Structure

SVG PNG

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SMILES

                    
CC/C(=C(\c1ccccc1)c1ccc(OCCN(C)C)cc1)c1ccccc1

                

                

                
                

                    
InChI

                    
InChI=1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-

                

                

                

                    
                    

                        
Molecular Formula

                        
C26H29NO

                    

                    
                    

                        
HBD / HBA

                        
- / 2

                    

                    
                    

                        
Rotatable Bonds

                        
8

                    

                    
                    
                    

                        
Heavy Atoms

                        
28

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            PPARG (Peroxisome Proliferator-Activated Receptor Gamma)
                            Antagonist
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            SIGMAR1 (Sigma-1 Receptor)
                            Antagonist
                        

                        
                    

                    
                    

                        

                            CYP2D6 (Cytochrome P450 2D6)
                            Substrate
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Major


                            
                                Tamoxifen + Warfarin
                            
                        

                        
                        
Tamoxifen dramatically increases warfarin anticoagulation, causing large INR elevations and a substantially elevated risk of serious bleeding.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Frequently Asked Questions

                

                    
                    

                        
                        

                            
This medication blocks estrogen receptors in breast tissue and is widely used to treat and reduce the risk of hormone receptor-positive breast cancer in both women and men. It is typically taken as a daily tablet for five to ten years as part of a long-term cancer prevention or treatment plan. Regular gynecologic check-ups are recommended because it can have estrogen-like effects on the uterus.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selective estrogen receptor modulator (SERM).

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Tamoxifen: Half-life: 5-7 days.

                        

                    

                    

                    

                        
                        

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

                        

                    

                

            

            

            
            
            

                
                
                    ADME Journey →
                
                
                
            

            

            
            
            

                
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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

    
    
        
        
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                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL83.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 2733526.
                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.