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Tacrolimus

CHEMBL3989887 Phase 4 Disetujui 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.

Berat Molekul

804,0180 g/mol

LogP

2,70

TPSA

178,00 Ų

Lipinski RO5

Gagal

Area Terapeutik

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

Kelas Obat

L — L - Antineoplastic and Immunomodulating Agents

Mekanisme Kerja

Calcineurin inhibitor binding FKBP12; suppresses IL-2 transcription.

Pharmacokinetics (PK)

Half-Life 12 hours

Pharmacodynamics (PD)

Mekanisme

Calcineurin inhibitor binding FKBP12; suppresses IL-2 transcription.

Struktur 2D

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

                    

                    
                    

                        
Ikatan yang Dapat Dirotasi

                        
7

                    

                    
                    
                    

                        
Atom Berat

                        
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.

    



                
            


            
            
            

                
Pertanyaan yang Sering Diajukan

                

                    
                    

                        
                        

                            
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.




        


        
        
    


    



    
Penyangkalan Medis

    

        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.