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Tacrolimus

CHEMBL3989887 Phase 4 已批准 Small molecule
Half-Life
12 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
804.0 g/mol
LogP
2.7
Phase
4

Binding the intracellular protein FKBP12, tacrolimus forms a complex that inhibits calcineurin and, in turn, blocks the transcription of interleukin-2. Cutting off this signal prevents T cells from activating, which is why the drug is used to stop the body from rejecting a transplanted kidney, liver, or heart. The same immune restraint also treats stubborn inflammatory skin conditions such as eczema. A large macrolide-type molecule (C44H69NO12) with a half-life of about 12 hours, it is a potent calcineurin inhibitor whose blood levels and effect on kidney function are tracked closely during treatment. By targeting the specific pathway of T-cell activation, it suppresses immunity selectively rather than broadly. Tacrolimus is an approved immunosuppressant that is a mainstay of solid-organ transplantation.

This medication suppresses the immune system to prevent the body from rejecting a transplanted organ such as a kidney, liver, or heart. It is also used to treat certain immune-related skin conditions like eczema when other treatments have not worked. Regular blood tests are needed to monitor drug levels and kidney function.

分子量

804.0180 g/mol

LogP

2.70

TPSA

178.00 Ų

Lipinski 五规则

不符合

治疗领域

Cardiovascular Disease Age-Related Macular Degeneration Non-Small Cell Lung Cancer Rheumatoid Arthritis Asthma Immunology Infectious Disease Melanoma Inflammatory Bowel Disease Psoriasis Systemic Lupus Erythematosus Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Lymphoma Transplant Medicine Type 2 Diabetes Hypertension Breast Cancer Atopic Dermatitis Hepatitis C Prostate Cancer Leukemia

药物分类

L — L - Antineoplastic and Immunomodulating Agents

作用机制

Calcineurin inhibitor binding FKBP12; suppresses IL-2 transcription.

Pharmacokinetics (PK)

Half-Life 12 hours

Pharmacodynamics (PD)

机制

Calcineurin inhibitor binding FKBP12; suppresses IL-2 transcription.

二维结构

SVG PNG

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SMILES

                    
C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC.O

                

                

                
                

                    
InChI

                    
InChI=1S/C44H69NO12.H2O/c1-10-13-31-19-25(2)18-26(3)20-37(54-8)40-38(55-9)22-28(5)44(52,57-40)41(49)42(50)45-17-12-11-14-32(45)43(51)56-39(29(6)34(47)24-35(31)48)27(4)21-30-15-16-33(46)36(23-30)53-7;/h10,19,21,26,28-34,36-40,46-47,52H,1,11-18,20,22-24H2,2-9H3;1H2/b25-19+,27-21+;/t26-,28+,29+,30-,31+,32-,33+,34-,36+,37-,38-,39+,40+,44+;/m0./s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C44H69NO12

                    

                    
                    

                        
HBD / HBA

                        
3 / 12

                    

                    
                    

                        
可旋转键数

                        
7

                    

                    
                    
                    

                        
重原子数

                        
57

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            MTOR (Mechanistic Target of Rapamycin)
                            Other
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            CYP3A4 (Cytochrome P450 3A4)
                            Substrate
                        

                        
                    

                    
                    

                        

                            ABCB1 (P-glycoprotein)
                            Substrate
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Moderate


                            
                                Tacrolimus + Trimethoprim
                            
                        

                        
                        
Trimethoprim impairs renal potassium excretion and may inhibit tubular secretion of tacrolimus, collectively increasing the risk of hyperkalemia and tacrolimus nephrotoxicity.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Tacrolimus + Fluconazole
                            
                        

                        
                        
Fluconazole markedly inhibits CYP3A4-mediated tacrolimus metabolism, causing 2- to 4-fold elevations in tacrolimus trough levels and substantial risk of nephrotoxicity and neurotoxicity.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Tacrolimus + Cyclosporine
                            
                        

                        
                        
Concurrent use of cyclosporine and tacrolimus dramatically amplifies nephrotoxicity and is generally contraindicated; both agents independently cause renal vasoconstriction and tubular injury.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Tacrolimus + Phenytoin
                            
                        

                        
                        
Phenytoin is a strong CYP3A4 inducer that can reduce tacrolimus exposure by more than 50%, putting transplant patients at risk for graft rejection.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Tacrolimus + Carbamazepine
                            
                        

                        
                        
Carbamazepine, a potent CYP3A4 inducer, substantially decreases tacrolimus blood concentrations, risking acute rejection in transplant recipients.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Tacrolimus + Metoprolol
                            
                        

                        
                        
Tacrolimus may mildly prolong the QT interval; metoprolol's bradycardic effect may compound this modestly, though clinically significant arrhythmia is uncommon at standard doses.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Tacrolimus + Omeprazole
                            
                        

                        
                        
Omeprazole inhibits CYP2C19 and weakly inhibits CYP3A4, leading to modest increases in tacrolimus exposure particularly in CYP2C19 poor metabolisers.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Tacrolimus + Diltiazem
                            
                        

                        
                        
Diltiazem inhibits CYP3A4 and P-glycoprotein, increasing tacrolimus blood concentrations by 40–70% and heightening the risk of dose-related tacrolimus toxicity.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
常见问题

                

                    
                    

                        
                        

                            
This medication suppresses the immune system to prevent the body from rejecting a transplanted organ such as a kidney, liver, or heart. It is also used to treat certain immune-related skin conditions like eczema when other treatments have not worked. Regular blood tests are needed to monitor drug levels and kidney function.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Calcineurin inhibitor binding FKBP12; suppresses IL-2 transcription.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Tacrolimus: Half-life: 12 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Tacrolimus 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

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL3989887.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 445643.
                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.