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# Microsomal triglyceride transfer protein (MTP) inhibitors

Oral drugs that stop the liver and gut from assembling VLDL and chylomicrons. Reserved for homozygous familial hypercholesterolaemia.

Updated Nov 1, 2026

## What they are

Lomitapide is the only member. It lowers LDL even when LDL receptors are absent, which is why it is used in homozygous familial hypercholesterolaemia (HoFH).

## Mechanism of action

Microsomal triglyceride transfer protein loads triglycerides onto apolipoprotein B inside the endoplasmic reticulum of hepatocytes and enterocytes. Blocking it prevents the assembly and secretion of VLDL (liver) and chylomicrons (gut), so less VLDL is made and less LDL is formed downstream, independent of LDL receptors.

Target: Microsomal triglyceride transfer protein (MTTP)

## Key points

- Works without LDL receptors: an option in homozygous FH.
- The lipid that is not exported stays in the liver: raised transaminases and fatty liver are the key risks (restricted programme).
- Fat that is not packaged stays in the gut: diarrhoea, nausea and abdominal pain, reduced by a strict low-fat diet.
- Metabolized by CYP3A4: strong inhibitors are contraindicated; grapefruit is avoided.
- Embryotoxic: pregnancy test and contraception.

## Drugs in this class

- [**Lomitapide** An oral MTP inhibitor that blocks VLDL and chylomicron assembly. Used with other lipid drugs in homozygous familial… Microsomal triglyceride transfer protein (MTP), large subunit](https://durgical.com/en/pharmacology/lomitapide/)

## Test yourself

Think of the answer, then tap the question to see it.

## Why does lomitapide work in homozygous FH when statins barely do?

It blocks VLDL assembly upstream, so it lowers LDL without needing LDL receptors.

## Why does lomitapide cause fatty liver?

Triglycerides that cannot be exported as VLDL accumulate in hepatocytes.

## What diet reduces lomitapide's gastrointestinal effects?

A strict low-fat diet.

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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: [Lomitapide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a614008.html) (MedlinePlus (U.S. National Library of Medicine), 2026).

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/classes/microsomal-triglyceride-transfer-protein-inhibitors/