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Lipid-lowering agent (microsomal triglyceride transfer protein inhibitor)

Juxtapid (lomitapide mesylate) is a prescription medicine used alongside a low-fat diet to help lower cholesterol levels in people with a rare genetic condition called homozygous familial hypercholesterolemia (HoFH). It works by blocking a specific protein that helps build certain types of fats in the body. Because it can affect liver health and how your body absorbs vitamins, it requires careful monitoring and specific supplement use.

How it worksJuxtapid blocks a protein called microsomal triglyceride transfer protein (MTP). This protein is needed to build the particles that carry cholesterol and fat through your blood; by blocking it, the drug helps lower cholesterol levels.

Brand names:JUXTAPID

Used for
Reducing low-density lipoprotein cholesterol (LDL-C)Reducing total cholesterol (TC)Reducing apo BReducing non-high-density lipoprotein cholesterol (non-HDL-C) in patients with homozygous familial hypercholesterolemia (HoFH)
Conditions
Homozygous familial hypercholesterolemia (HoFH)
Class
Lipid-lowering agentMTP inhibitorLipid-lowering agent (microsomal triglyceride transfer protein inhibitor)Hepatic (Liver)Gastrointestinal

How to take

FormsOral capsule
RoutesOral

Treatment usually starts at 5 mg once daily. The dose is gradually increased by a doctor over several weeks, potentially up to a maximum of 60 mg daily.

You must take daily supplements of vitamin E, linoleic acid, alpha-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA) because this medicine can reduce your absorption of these fats and vitamins. These supplements should be taken once daily, whole, with water, and without food, at least 2 hours after your evening meal.

Key warnings

Juxtapid can cause increases in liver enzymes (transaminases) and can increase the amount of fat in your liver (hepatic steatosis).

  • ·Juxtapid can cause increases in liver enzymes (transaminases) and can increase the amount of fat in your liver (hepatic steatosis).
  • ·Risk of liver damage (hepatotoxicity)
  • ·Risk of harm to an unborn baby (embryo-fetal toxicity)
  • ·Interference with the absorption of other oral medications due to stomach issues

Do not use if

  • ·Pregnancy
  • ·Moderate or severe liver disease
  • ·Active liver disease
  • ·Use with strong or moderate CYP3A4 inhibitors

Side effects

Common

DiarrheaNauseaVomitingIndigestion (dyspepsia)Abdominal pain

Serious

  • ·Liver problems (increased liver enzymes or increased fat in the liver)
  • ·Reduced absorption of fat-soluble vitamins
  • ·Fetal harm if taken during pregnancy

Seek help if

  • ·Signs of liver issues
  • ·Pregnancy

Interactions

  • ·Strong or moderate CYP3A4 inhibitors (these can significantly increase Juxtapid levels in your body)
  • ·Grapefruit juice (must be avoided)
  • ·Warfarin (Juxtapid may increase the amount of warfarin in your blood)
  • ·Simvastatin and lovastatin (may increase the risk of muscle problems)
  • ·Bile acid sequestrants (should be taken at least 4 hours apart from Juxtapid)
  • ·Weak CYP3A4 inhibitors (may require a dose reduction)
FoodMust be taken as part of a low-fat diet. Avoid grapefruit juice. Supplements should be taken at least 2 hours after the evening meal.

Special populations

PregnancyJuxtapid should not be used during pregnancy as it may cause harm to the fetus. Women of reproductive potential should use effective birth control and obtain a negative pregnancy test before starting treatment.

PediatricThe safety and effectiveness of Juxtapid have not been tested in children.

GeriatricThere is not enough information to know if older adults respond differently, but doctors should use caution when prescribing it to elderly patients due to potential changes in liver or kidney function.

Talk to your doctor

Monitor

  • ·Liver enzymes (ALT, AST)
  • ·Alkaline phosphatase
  • ·Total bilirubin
  • ·Vitamin E and fatty acid levels
  • ·INR (if taking warfarin)

Questions to ask

  • ·How often will my liver enzymes be monitored?
  • ·Which vitamin supplements should I take with Juxtapid?
  • ·How will Juxtapid interact with my other medications?
  • ·What is the best time of day to take my dose?

Pharmacokinetics

BioavailabilityApproximately 7%
Protein binding99.8% plasma-protein bound
MetabolismExtensively metabolized by the liver, including oxidation, oxidative N-dealkylation, glucuronide conjugation, and piperidine ring opening via CYP3A4.

Practical

OverdoseThere is no specific treatment for an overdose. Patients should be treated based on their symptoms and their liver function should be monitored.

StorageStore between 68°F and 77°F (20°C to 25°C). Keep the container tightly closed and protect from moisture.

Ingredients

Allergens

lactose

Inactive

pregelatinized starchsodium starch glycolatemicrocrystalline celluloselactose monohydratesilicon dioxidemagnesium stearategelatintitanium dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.