Lomitapide

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Information about Lomitapide

Lomitapide is a cholesterol lowering agent that acts by inhibition of the microsomal triglyceride transfer protein and is used to treat the severe lipid abnormalities of familial hypercholesterolemia. Lomitapide is associated with mild, asymptomatic and self-limited serum aminotransferase elevations during therapy that are usually accompanied by an increase in hepatic fat. Long term therapy with lomitapide has been linked to development of steatohepatitis and hepatic fibrosis.

Mechanism of action of Lomitapide

Lomitapide (loe mi' ta pide) is a potent, orally available inhibitor of the hepatic microsomal triglyceride transfer protein (MTTP) and is used to treat severe forms of familial hypercholesterolemia. MTTP is responsible for transferring triglyceride to apolipoprotein B in the liver which is necessary for the assembly of very low density lipoproteins, the precursors of low density lipoproteins (LDL). Inhibition of apolipoprotein B assembly leads to a marked decrease in circulating LDL cholesterol and triglycerides. Lomitapide is typically used in combination with statins.

FDA approval information for Lomitapide

Lomitapide was approved for use in the United States in 2012, but its indications were limited to patients with homozygous familial hypercholesterolemia. Use of lomitapide can be associated with serum aminotransferase elevations and increase in hepatic fat. Because of the risk of liver injury, lomitapide is available only as a part of a "Risk Evaluation and Mitigation Strategy" [REMS] that requires regular monitoring of liver tests.

Dosage and administration for Lomitapide

Lomitapide is available in capsules of 5, 10, 20, 30, 40 and 60 mg under the trade name Juxtapid.

The recommended dose is 5 mg daily initially, with subsequent increases based upon tolerance and effectiveness to a maximum of 60 mg daily.

Side effects of Lomitapide

Side effects are not uncommon and include diarrhea, nausea, dyspepsia and abdominal pain that are ameliorated and partially prevented by strict adherence to a low fat diet. Lomitapide can also cause marked drug-drug interactions and increase toxicities of other medications (statins, warfarin, antibiotics). Chronic use of lomitapide can result in fat-soluble vitamin malabsorption and deficiencies.

Lipid lowering medications

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