Active Ingredient History
Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes. Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Combination drugs
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Metabolic Diseases (approved 2002)
Acute Coronary Syndrome (Phase 4)
Acute Kidney Injury (Phase 1)
Alopecia Areata (Phase 1)
Aortic Valve Stenosis (Phase 3)
Atherosclerosis (Phase 4)
Atrial Fibrillation (Phase 4)
Cardiovascular Diseases (Phase 4)
Cholesterol (Phase 3)
Coronary Artery Disease (Phase 4)
Coronary Disease (Phase 4)
Diabetes Mellitus (Phase 4)
Diabetes Mellitus, Type 1 (Phase 4)
Diabetes Mellitus, Type 2 (Phase 4)
Diabetic Nephropathies (Phase 3)
Diabetic Neuropathies (Phase 2)
Drug Interactions (Phase 1)
Dyslipidemias (Phase 4)
Endocrine System Diseases (Phase 4)
Essential Hypertension (Phase 3)
Healthy Volunteers (Phase 4)
Heart Diseases (Phase 4)
Heart Failure, Diastolic (Phase 4)
Heart Transplantation (Phase 3)
Hemostasis (Phase 4)
Hepatitis C (Phase 4)
Hepatitis C, Chronic (Phase 2)
Hepatitis D, Chronic (Phase 2)
HIV (Phase 4)
HIV Infections (Phase 4)
Homozygous Familial Hypercholesterolemia (Phase 3)
Hyperlipoproteinemia Type II (Phase 3)
Hypertension (Phase 4)
Hypertriglyceridemia (Phase 3)
Immunosuppression Therapy (Phase 1)
Inflammation (Phase 4)
Intestinal Neoplasms (Phase 1)
Ischemic Stroke (Phase 4)
Kidney Diseases (Phase 4)
Kidney Transplantation (Phase 3)
Lipid Metabolism Disorders (Phase 4)
Lipid Metabolism, Inborn Errors (Phase 3)
Lipidoses (Phase 2)
Lipoproteins (Phase 4)
Lung Transplantation (Phase 3)
Magnetic Resonance Imaging (Phase 4)
Metabolic Syndrome (Phase 4)
Metabolism (Phase 1)
Metabolism, Inborn Errors (Phase 3)
Myocardial Infarction (Phase 4)
Neuropsychology (Phase 4)
Non-alcoholic Fatty Liver Disease (Phase 4)
Non-ST Elevated Myocardial Infarction (Phase 4)
Nutritional and Metabolic Diseases (Phase 4)
Oxidative Stress (Phase 2)
Peripheral Arterial Disease (Phase 4)
Pharmacokinetics (Phase 1)
Primary Prevention (Phase 4)
Prostatic Neoplasms (Early Phase 1)
Renal Insufficiency, Chronic (Phase 4)
ST Elevation Myocardial Infarction (Phase 4)
Stroke (Phase 4)
Therapeutic Equivalency (Phase 1)
Transplants (Phase 4)
Vascular Calcification (Phase 4)
Vascular Diseases (Phase 4)
Vitamin D Deficiency (Phase 4)
Trial | Phase | Start Date | Organizations | Indications |
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