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Synonyms: Crestor® | ZD4522
rosuvastatin is an approved drug (FDA (2003))
Compound class: Synthetic organic
Comment: Marketed formulations may contain rosuvastatin calcium (PubChem CID 5282455).
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: rosuvastatin
|No information available.|
|Summary of Clinical Use|
|Used in the treatment of primary hyperlipidemia, mixed dyslipidemia and hypertriglyceridemia.
The US FDA approved marketing of the first generic version of rosuvastatin calcium in May 2016. Rosuvastatin is approved in fixed-dose combination with ezetimibe (Roszet™) as an adjunct to diet, to reduce LDL-C levels in adult patients with primary non-familial hyperlipidemia or with homozygous familial hypercholesterolemia.
|Mechanism Of Action and Pharmacodynamic Effects|
|Competitive inhibitor of HMG-CoA reductase, the enzyme catalysing the rate-limiting step of cholesterol synthesis. Acting primarily in the liver, rosuvastatin decreases hepatic cholesterol concentrations. For a complete overview of the mechanism of action of this drug, please see the entry on DrugBank linked to from this ligand page.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)