Synonyms: Lipitor®
atorvastatin is an approved drug (FDA (1996))
Compound class:
Synthetic organic
Comment: The 3S, 5S-Atorvastatin enantiomer is inactive [4]. 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 ChartsThese 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 |
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References |
1. Carbonell T, Freire E. (2005)
Binding thermodynamics of statins to HMG-CoA reductase. Biochemistry, 44 (35): 11741-8. [PMID:16128575] |
2. Flockhart DA.
Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed on 18/11/2014. Modified on 18/11/2014. http://medicine.iupui.edu/clinpharm/ddis/clinical-table/ |
3. Istvan ES, Deisenhofer J. (2001)
Structural mechanism for statin inhibition of HMG-CoA reductase. Science, 292 (5519): 1160-4. [PMID:11349148] |
4. Kocarek TA, Dahn MS, Cai H, Strom SC, Mercer-Haines NA. (2002)
Regulation of CYP2B6 and CYP3A expression by hydroxymethylglutaryl coenzyme A inhibitors in primary cultured human hepatocytes. Drug Metab Dispos, 30 (12): 1400-5. [PMID:12433810] |
5. McTaggart F, Buckett L, Davidson R, Holdgate G, McCormick A, Schneck D, Smith G, Warwick M. (2001)
Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am J Cardiol, 87 (5A): 28B-32B. [PMID:11256847] |