Pharmacology · Class
Cholesterol absorption inhibitors !
Drugs that block cholesterol uptake in the small intestine. Ezetimibe is the usual add-on when a statin alone does not reach the LDL goal.
Updated 2026-11-01
What they are
Oral lipid-lowering drugs that act on the intestinal sterol transporter NPC1L1. Ezetimibe is the only one in wide use, alone or with a statin.
Mechanism of action
NPC1L1 at the brush border of jejunal enterocytes takes up dietary and biliary cholesterol and plant sterols. Blocking it means fewer chylomicrons carry cholesterol to the liver; hepatic cholesterol falls and LDL receptors rise, so blood LDL falls. The liver compensates by making more cholesterol, which is why combining with a statin works so well.
Target: NPC1L1 sterol transporter (Niemann-Pick C1-Like 1) of the intestinal brush border
Drugs in this class
Test yourself
Think of the answer, then tap the question to see it.
Why does ezetimibe work better combined with a statin than alone?
Blocking absorption makes the liver synthesize more cholesterol; the statin blocks that compensatory synthesis.
Where is NPC1L1 and what does it carry?
On the brush border of small-intestine enterocytes; it takes up cholesterol and plant sterols from the gut lumen.
Which lipid drug must be separated in time from ezetimibe?
A bile acid sequestrant such as colestyramine, which binds ezetimibe and lowers its absorption.
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - EZETIMIBE tablet (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 37 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.