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[Pharmacology](https://durgical.com/en/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

## Key points

- Ezetimibe lowers LDL moderately alone and adds to a statin; it is the usual first add-on before PCSK9 inhibitors.
- It is glucuronidated and recirculates through the bile (enterohepatic cycle), which gives it a long half-life.
- Bile acid sequestrants bind it: they are separated in time.
- Also used in sitosterolemia, a rare disease of plant-sterol overabsorption.
- Generally well tolerated; with a statin, the statin's warnings (muscle, liver) still apply.

## Drugs in this class

- [**Ezetimibe** Blocks cholesterol absorption in the gut. Added to a statin it lowers LDL further; it is the usual first add-on to a… NPC1L1 sterol transporter](https://durgical.com/en/pharmacology/ezetimibe/)

## 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.

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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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c37c695b-fb40-423c-9b73-d1aa58a34db9) (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](https://atcddd.fhi.no/atc_ddd_index/?code=C10AX) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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