💊 Fármacos A-Z 🧬 Dianas 🛠 Herramientas 📚 Guías
Todos los fármacos Clases de fármacos Áreas terapéuticas Efectos Secundarios
Guías Glosario Línea de tiempo
Comparaciones Recorridos de fármacos Familias farmacológicas
🇺🇸 English 🇰🇷 한국어 🇯🇵 日本語 🇨🇳 中文简体 🇪🇸 Español 🇧🇷 Português 🇮🇳 हिन्दी 🇸🇦 العربية 🇫🇷 Français 🇷🇺 Русский 🇩🇪 Deutsch 🇹🇷 Türkçe 🇻🇳 Tiếng Việt 🇮🇩 Bahasa Indonesia 🇹🇭 ไทย

Cerivastatin

CHEMBL1477 Phase 4 Aprobado Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
459.5 g/mol
LogP
3.6
Phase
4

Withdrawal in 2001 makes cerivastatin one of the most cited cases in post-marketing drug safety. The compound is a synthetic inhibitor of HMG-CoA reductase, the rate-limiting enzyme of the mevalonate pathway; blocking it depletes intracellular cholesterol, upregulates LDL receptor expression and lowers circulating LDL cholesterol, the mechanism shared by the statin class. Efficacy was not the problem. An unacceptably high incidence of potentially fatal rhabdomyolysis emerged after marketing, concentrated among patients also receiving gemfibrozil, and the manufacturer removed the drug from the world market voluntarily. The molecule is C26H34FNO5 with a mass near 459.5 g/mol, and its development had reached the final clinical phase.

A synthetic HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk. It was voluntarily withdrawn from the worldwide market in 2001 due to an unacceptably high incidence of potentially fatal rhabdomyolysis, particularly when combined with gemfibrozil. It represents an important pharmacovigilance case study in post-marketing drug safety.

Peso molecular

459,5000 g/mol

LogP

3,60

TPSA

99,90 Ų

Regla de cinco de Lipinski

Cumple

Áreas terapéuticas

Hiperlipidemia

Mecanismo de acción

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.

Estructura 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C26H34FNO5/c1-15(2)25-21(11-10-19(29)12-20(30)13-23(31)32)24(17-6-8-18(27)9-7-17)22(14-33-5)26(28-25)16(3)4/h6-11,15-16,19-20,29-30H,12-14H2,1-5H3,(H,31,32)/b11-10+/t19-,20-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C26H34FNO5

                    

                    
                    

                        
HBD / HBA

                        
3 / 7

                    

                    
                    

                        
Enlaces Rotables

                        
11

                    

                    
                    
                    

                        
Átomos Pesados

                        
33

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Preguntas frecuentes

                

                    
                    

                        
                        

                            
A synthetic HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk. It was voluntarily withdrawn from the worldwide market in 2001 due to an unacceptably high incidence of potentially fatal rhabdomyolysis, particularly when combined with gemfibrozil. It represents an important pharmacovigilance case study in post-marketing drug safety.

                        

                    

                    

                    

                    
                    

                        
                        

                            
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, Cerivastatin 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).
                CHEMBL1477.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 446156.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
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.