Last reviewed 2026-04-20 · How we verify

Lipitor (atorvastatin)

Selective competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis.

Atorvastatin is an HMG-CoA reductase inhibitor indicated to reduce cardiovascular risk in multiple patient populations including those with CHD, diabetes, and familial hypercholesterolemia, as well as to reduce LDL-C levels. The drug demonstrates moderate bioavailability of 14% for parent compound but 30% for active inhibitory activity, with extensive hepatic metabolism via CYP3A4 and a long half-life of 20-30 hours for inhibitory activity. Significant drug interactions exist with CYP3A4 inhibitors (cyclosporine, gemfibrozil, antivirals) that substantially increase atorvastatin exposure and myopathy risk, requiring careful management or avoidance. Atorvastatin is contraindicated in acute liver failure or decompensated cirrhosis and in patients with hypersensitivity to the drug.

At a glance

Mechanism of action

Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols including cholesterol. In animal models, atorvastatin lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL. Atorvastatin also reduces LDL production and the number of LDL particles.

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

• Nasopharyngitis
• Arthralgia
• Diarrhea
• Pain in extremity
• Urinary tract infection
• Dyspepsia
• Nausea
• Musculoskeletal pain
• Muscle spasms
• Myalgia
• Insomnia
• Pharyngolaryngeal pain

Drug interactions

• Cyclosporine or Gemfibrozil
• Anti-Viral Medications
• Rifampin
• Oral Contraceptives
• Digoxin

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

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Lipitor CI brief — competitive landscape report
• Lipitor updates RSS · CI watch RSS
• Pfizer Inc. portfolio CI