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Description: Atorvastatin (Lipitor) is a member of the drug class known as statins. It is used for lowering cholesterol. Atorvastatin inhibits the rate-determining enzyme located in hepatic tissue that produces mevalonate, a small molecule used in the synthesis of cholesterol and other mevalonate derivatives. This lowers the amount of cholesterol produced which in turn lowers the total amount of LDL cholesterol. Atorvastatin is a competitive inhibitor of HMG-CoA reductase.
Drug Type: Small Molecule; Approved
Pharmacology: Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor, is used to lower cholesterol and triglycerides in patients with hypercholesterolemia and mixed dyslipidemia and in the treatment of homozygous familial hypercholesterolemia. Atorvastatin has a unique structure, long half-life, and hepatic selectivity, explaining its greater LDL-lowering potency compared to other HMG-CoA reductase inhibitors.
Mechanism of Action: Atorvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol, and a subsequent decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol.
Indication: For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia.
Half Life: 14 hours
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Individual Studies
  • Endothelial cells and atorvastatin

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Rationale: Immortalized cells may exhibit important differences relative to their primary cell counterparts. Microarrays were used compare primary human umbilical vein endothelial cells (HUVECs) and the immortalized HUVEC cell line EA.hy926, in their response to inhibition of the mevalonate pathway …

    Authors: Boerma M, Burton GR, Wang J et al.

    Organization: University of Arkansas for Medical Scien…

  • Three primary human cell lines treated with atorvastatin or an inhibitor of Rho kinase

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Inhibitors of Rho kinase (ROCK) are a new class of drugs with potential benefit in oncology, neurology, and fibrotic and cardiovascular diseases. ROCK inhibitors modulate many cellular functions, some of which are similar to the pleiotropic (non-lipid lowering) effects of statins, suggesting additiv…

    Authors: Boerma M, Loose DS, Hauer-Jensen M

    Organization: University of Arkansas for Medical Scien…

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Thought leaders and organizations working on research involving atorvastatin.

  • Nanette K Wenger
  • Giuseppe Patti
  • John J P Kastelein
  • Germano Di Sciascio
  • Vera Bittner
  • Pfizer
  • National Institute of Allergy and Infectious Diseases (NIAID)
  • University of Oslo School of Pharmacy
  • Bayside Health
  • Beth Israel Deaconess Medical Center
  • University of Pennsylvania
  • University of California
  • Stanford University
  • Leiden University Medical Center
  • Gachon University

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