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Rosuvastatin

CHEMBL1496 Phase 4 Approuvé Small molecule
Half-Life
19 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
481.5 g/mol
LogP
1.6
Phase
4

Among the statins, rosuvastatin is noted for potency at low doses, competitively inhibiting HMG-CoA reductase and thereby the rate-limiting step of cholesterol biosynthesis. The consequence is a marked reduction in LDL cholesterol and triglycerides with a rise in HDL cholesterol, and that lipid change translates into lower rates of myocardial infarction, stroke and other cardiovascular events. General tolerability combined with efficacy at modest doses accounts for its position among the most widely prescribed lipid-lowering agents. An elimination half-life near 19 hours is long for the class and supports once-daily use. The compound is a cardiovascular-system agent with formula C22H28FN3O6S and a mass close to 481.5 g/mol.

A potent statin medication used to lower LDL cholesterol and triglycerides while raising HDL cholesterol, significantly reducing the risk of heart attack, stroke, and other cardiovascular events. It is generally well-tolerated and effective at low doses, making it one of the most widely prescribed cholesterol-lowering medications.

Masse moléculaire

481,5390 g/mol

LogP

1,60

TPSA

149,00 Ų

Règle des 5 de Lipinski

Conforme

Aires thérapeutiques

Neurology Cardiovascular Disease Stroke Hyperlipidemia

Classes de médicaments

C — C - Cardiovascular System

Mécanisme d'action

Competitive inhibitor of HMG-CoA reductase.

Pharmacokinetics (PK)

Half-Life 19 hours

Pharmacodynamics (PD)

Mécanisme

Competitive inhibitor of HMG-CoA reductase.

Structure 2D

SVG PNG

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SMILES

                    
CC(C)c1nc(N(C)S(C)(=O)=O)nc(-c2ccc(F)cc2)c1/C=C/[C@@H](O)C[C@@H](O)CC(=O)O

                

                

                
                

                    
InChI

                    
InChI=1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C22H28FN3O6S

                    

                    
                    

                        
HBD / HBA

                        
3 / 10

                    

                    
                    

                        
Liaisons Rotatives

                        
10

                    

                    
                    
                    

                        
Atomes Lourds

                        
33

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            HMGCR (HMG-CoA Reductase)
                            Inhibitor
                        

                        
                        Primary Target
                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Moderate


                            
                                Rosuvastatin + Warfarin
                            
                        

                        
                        
Rosuvastatin increases warfarin plasma concentrations through inhibition of CYP2C9, potentially leading to supratherapeutic INR values.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Rosuvastatin + Colchicine
                            
                        

                        
                        
Rosuvastatin and colchicine share BCRP transporter-mediated elimination; colchicine may weakly increase rosuvastatin exposure, and both carry myotoxic potential that could be additive.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Foire aux questions

                

                    
                    

                        
                        

                            
A potent statin medication used to lower LDL cholesterol and triglycerides while raising HDL cholesterol, significantly reducing the risk of heart attack, stroke, and other cardiovascular events. It is generally well-tolerated and effective at low doses, making it one of the most widely prescribed cholesterol-lowering medications.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitive inhibitor of HMG-CoA reductase.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Rosuvastatin: Half-life: 19 hours.

                        

                    

                    

                    

                        
                        

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

                        

                    

                

            

            

            
            
            

                
                
                    ADME Journey →
                
                
                
            

            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Atorvastatin
                            Small molecule
                        
                        
                        
                            Amlodipine
                            Small molecule
                        
                        
                        
                            Lisinopril
                            Small molecule
                        
                        
                        
                            Metoprolol
                            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).
                CHEMBL1496.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 446157.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-08-20.




        


        
        
    


    



    
Avertissement médical

    

        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.