Last reviewed 2026-04-19 · How we verify

Lipitor (Atorvastatin Calcium)

Lipitor is a selective, competitive inhibitor of HMG-CoA reductase, a key enzyme in cholesterol synthesis.

Lipitor, developed by Pfizer Inc., is a statin medication used to prevent cardiovascular disease and treat abnormal lipid levels. It works by inhibiting HMG-CoA reductase, a key enzyme in cholesterol synthesis. Lipitor is a first-line treatment for reducing cholesterol and is taken orally. The medication is effective in lowering plasma cholesterol and lipoprotein levels. It is used to treat conditions such as angina pectoris, arteriosclerotic vascular disease, and familial hypercholesterolemia. Lipitor has been widely used and has a significant commercial presence, with revenue of $63.6 billion. Its mechanism of action and clinical efficacy have made it a key medication in the treatment of cardiovascular disease.

At a glance

Mechanism of action

Lipitor works by inhibiting the enzyme HMG-CoA reductase, which is responsible for converting 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. This inhibition leads to a decrease in cholesterol synthesis in the liver and an increase in the number of hepatic LDL receptors on the cell surface, enhancing the uptake and catabolism of LDL. As a result, Lipitor lowers plasma cholesterol and lipoprotein levels, making it an effective treatment for conditions such as high cholesterol and cardiovascular disease.

Approved indications

• Angina pectoris
• Arteriosclerotic vascular disease
• Cerebrovascular accident
• Familial hypercholesterolemia - heterozygous
• Familial hypercholesterolemia - homozygous
• Familial type 3 hyperlipoproteinemia
• Hypercholesterolemia
• Hypertriglyceridemia
• Mixed hyperlipidemia
• Myocardial Infarction Prevention
• Primary Prevention of Coronary Heart Disease
• Prinzmetal angina
• Slow Progression of Coronary Artery Disease

Common side effects

• Myopathy and Rhabdomyolysis
• Immune-Mediated Necrotizing Myopathy
• Hepatic Dysfunction
• Increases in HbA1c and Fasting Serum Glucose Levels
• Nasopharyngitis
• Arthralgia
• Diarrhea
• Pain in extremity
• Urinary tract infection
• Dyspepsia
• Nausea
• Musculoskeletal pain

Drug interactions

• P-glycoprotein Substrates
• atazanavir
• ciclosporin
• clarithromycin
• darunavir
• delavirdine
• diltiazem
• dronedarone
• erythromycin
• fenofibrate
• fluconazole
• fosamprenavir

Key clinical trials

• Atorvastatin Therapy in the Treatment of Dyslipidemia in Children With Steroid Sensitive Nephrotic Syndrome (PHASE4)
• Atorvastatin Therapy on Xanthoma in Alagille Syndrome (PHASE4)
• Atorvastatin in Active Vitiligo (PHASE2)
• A Prospective, Open, Observational Study to Confirm the Lipid-lowering Effect, Changes in Glucose Metabolism, and Safety After 6 Months of Administration of Atostazet to Hypercholesterolemic Patients 65 Years of Age or Older
• A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events (PHASE3)
• Cholesterol Disruption in Combination With the Standard of Care in Patients With Advanced Pancreatic Adenocarcinoma (EARLY_PHASE1)
• Statin and Vitamin D Treatment in Patients With Thyroid Eye Disease (NA)
• Metformin Alleviates Abnormal Glucose Metabolism Induced by Statins in Schizophrenia Patients (PHASE3)

Patents

Primary sources

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