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atorvastatin is an approved drug (FDA (1996))
Compound class: Synthetic organic
Comment: The 3S, 5S-Atorvastatin enantiomer is inactive . Atorvastatin is metabolised to form active metabolites atorvastatin lactone (CID 6483036), o-hydroxyatorvastatin (CID 9808225) and p-hydroxyatorvastatin (CID 9851106).
Atorvastatin calcium is found in combination with amlodipine besylate in the drug Caduet®.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: atorvastatin
|No information available.|
|Summary of Clinical Use|
|Cholesterol-lowering drug used to treat hypercholesterolaemia and mixed lipidemia, and as a primary preventative medication for patients with multiple risk factors for coronary heart disease. Atorvastatin is a component of the fixed-ratio drug Caduet® (marketed as Envacar® in some countries) which also contains the calcium channel blocker amlodipine. Caduet® was first approved by the US FDA in 2004.|
|Mechanism Of Action and Pharmacodynamic Effects|
|Atorvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway.|