lomitapide mesylate at a glance
Medicine class
Microsomal triglyceride transfer protein inhibitor
Licensed use
Additional treatment for adults with homozygous familial hypercholesterolaemia
Administration
Swallow the capsule with water on an empty stomach after the evening meal; avoid grapefruit juice.
Specialist oversight
Treatment is initiated and monitored by a clinician experienced in lipid disorders.
What is lomitapide mesylate used for?
The licensed indication is:
As an addition to a low-fat diet and other lipid-lowering treatments, with or without LDL apheresis, in adults with homozygous familial hypercholesterolaemia. Genetic confirmation should be obtained whenever possible, and other causes of high cholesterol excluded.
How does lomitapide mesylate work?
Lomitapide blocks microsomal triglyceride transfer protein in the liver and intestine. This reduces assembly and release of apolipoprotein B-containing particles, lowering circulating LDL cholesterol and triglycerides.
lomitapide mesylate preparations and strengths
Capsule
Route: Oral
Strengths: 5 mg, 10 mg, 20 mg
How to take lomitapide mesylate
Follow the specialist’s instructions and do not change treatment yourself.
Swallow the capsule with water on an empty stomach after the evening meal.
Continue the prescribed low-fat diet; this helps reduce gastrointestinal effects.
Avoid grapefruit juice and alcohol.
Take the advised vitamin E and essential fatty-acid supplements.
Tell the specialist or pharmacist before starting, stopping or changing any other medicine or herbal product.
lomitapide mesylate side effects
Common or expected effects
- Diarrhoea, nausea or vomiting
- Abdominal pain, discomfort or bloating
- Indigestion, wind or constipation
- Reduced appetite and weight loss
- Headache, dizziness or tiredness
- Raised liver enzymes or fatty liver
Get urgent medical advice
- Yellow skin or eyes, fever, flu-like symptoms, unusual tiredness or abdominal pain suggesting liver injury
- Persistent or severe diarrhoea or vomiting causing dehydration
- Unexplained muscle pain, tenderness or weakness, particularly when also taking a statin
- Vomiting blood, rectal bleeding or blood in the stool
lomitapide mesylate in pregnancy
Lomitapide is contraindicated during pregnancy because animal studies found developmental harm and reliable human data are unavailable. Pregnancy should be excluded before treatment and effective contraception used; anyone who becomes pregnant should stop taking it and contact their specialist immediately.
lomitapide mesylate while breastfeeding
It is unknown whether lomitapide enters human milk. The specialist should discuss whether breastfeeding or lomitapide should be discontinued, considering the treatment’s importance to the mother.
lomitapide mesylate interactions
Lomitapide has important interactions. Check all prescriptions, over-the-counter products, supplements and herbal remedies with the specialist or pharmacist.
Strong or moderate CYP3A4 inhibitors
Azole antifungals, clarithromycin, erythromycin, HIV protease inhibitors, diltiazem, verapamil and dronedarone can markedly increase lomitapide exposure and are contraindicated.
Grapefruit juice
Can substantially increase lomitapide exposure and should be avoided.
Weak CYP3A4 inhibitors, including atorvastatin
May increase lomitapide exposure, requiring specialist review of administration timing or treatment.
Common questions about lomitapide mesylate
Answers are fully visible for fast scanning and source review.
What is lomitapide mesylate used for?
It is licensed as additional treatment for adults with homozygous familial hypercholesterolaemia alongside a low-fat diet and other lipid-lowering treatments.
How does lomitapide mesylate lower cholesterol?
It blocks microsomal triglyceride transfer protein, reducing production and release of LDL-containing particles by the liver and intestine.
Why must lomitapide mesylate be taken without food?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.