Drug reference

Lomitapide

Statin · Hyperlipidaemia

StatinHyperlipidaemia

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

—

not curated

Top interactionssee all 12 →

LopinavirContraindicatedTextbookG&G 14e · p742
AbacavirSevereDatabaseDDInter
AbemaciclibSevereDatabaseDDInter
AbirateroneSevereDatabaseDDInter

Mechanism

Lomitapide inhibits microsomal triglyceride transfer protein (MTP), an enzyme essential for the lipidation and assembly of apolipoprotein B-containing lipoproteins (VLDL in the liver and chylomicrons in the intestine). By blocking MTP, it prevents VLDL secretion from hepatocytes, reducing circulating LDL cholesterol by 40-50% — even in patients with homozygous familial hypercholesterolemia who have no functional LDL receptors. Its use is restricted to homozygous FH because MTP inhibition causes hepatic triglyceride accumulation and steatosis, requiring regular liver monitoring and a strict low-fat diet.

Indications

Homozygous familial hypercholesterolaemiapatients who have not responded adequately to diet and other appropriate measuresAdjunct to diet for lowering LDL-C, total cholesterol, apo B, and non–HDL-C in patients with HoFH

Dosing

Adult: Initially 40 mg once daily, then increased if necessary up to 80 mg once daily, adjusted at intervals of at least 4 weeks, dose to be taken at night
Max dose: 80 mg once daily

Pharmacokinetics

Metabolism

Metabolized by CYP3A4

Contraindications

Inhibitors of CYP3A4
Women of childbearing potential (unless negative pregnancy test and effective contraception are used due to embryotoxicity)

Side effects

Common

Significant diarrheaVomitingAbdominal pain

Serious

Hepatotoxicity
Liver steatosis
Elevations in ALT or AST greater than three times the upper limit of normal

Drug interactions

Lopinavir

Contraindicated

Textbook

Increased risk of lomitapide adverse effects, particularly hepatotoxicity.

Lomitapide is contraindicated with inhibitors of CYP3A4.

Source: G&G 14e · p742

Abacavir

Severe

Database