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Cilastatin Sodium

CHEMBL1201057 Phase 4 Aprovado Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
380.4 g/mol
LogP
—
Phase
4

The sodium salt form of cilastatin is co-formulated with imipenem in the fixed combination product imipenem-cilastatin for intravenous administration. By blocking renal dehydropeptidase-I, it preserves adequate urinary concentrations of imipenem for treating urinary tract infections and reduces proximal tubule toxicity. The sodium content should be considered in patients requiring sodium restriction.

Peso Molecular

380,4000 g/mol

TPSA

158,00 Ų

Áreas Terapêuticas

Infectious Disease Ovarian Cancer Hematology Oncology Obesity Tuberculosis

Mecanismo de Ação

Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mecanismo

Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.

Estrutura 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
CC1(C)C[C@@H]1C(=O)N/C(=C\CCCCSC[C@H](N)C(=O)O)C(=O)[O-].[Na+]

                

                

                
                

                    
InChI

                    
InChI=1S/C16H26N2O5S.Na/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21;/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23);/q;+1/p-1/b12-6-;/t10-,11+;/m1./s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C16H25N2NaO5S

                    

                    
                    

                        
HBD / HBA

                        
3 / 7

                    

                    
                    

                        
Ligações Rotacionáveis

                        
11

                    

                    
                    
                    

                        
Átomos Pesados

                        
25

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Perguntas frequentes

                

                    
                    

                        
                        

                            
The sodium salt form of cilastatin is co-formulated with imipenem in the fixed combination product imipenem-cilastatin for intravenous administration. By blocking renal dehydropeptidase-I, it preserves adequate urinary concentrations of imipenem for treating urinary tract infections and reduces proximal tubule toxicity. The sodium content should be considered in patients requiring sodium restriction.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Cilastatin Sodium 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).
                CHEMBL1201057.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 23663403.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
Aviso Médico

    

        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.