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Lomitapide

Class
Hypolipidemic agents
Subclass
Microsomal triglyceride transfer protein inhibitors
Generic name
Lomitapide mesylate
Brand names
Juxtapid®
Common formulations
Capsule
Dosage and administration
Adults patients
Adjunctive treatment for homozygous familial hypercholesterolemia
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Start at: 5 mg PO daily for 2 weeks
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Maintenance: 5-60 mg PO daily
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Maximum: 60 mg per day
Taken at least 2 hours after the evening meal. Double the dose every 4 weeks based on response.
Indications for use
Labeled indications
Adults
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Adjunctive treatment for homozygous familial hypercholesterolemia
Safety risks
Boxed warnings
Hepatotoxicity
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Maintain a high level of suspicion, as lomitapide has been associated with increases in serum transaminase levels and hepatic fat. Measure serum transaminases, ALP, and TBIL before initiating lomitapide and monitor serum transaminases regularly during treatment.
Contraindications
Hypersensitivity to lomitapide or its components
Total lactose deficiency or glucose-galactose malabsorption
Concomitant use of moderate or strong CYP3A4 inhibitors
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Eliminate grapefruit juice from diet while taking lomitapide.
Warnings and precautions
Bleeding
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Use caution in patients taking warfarin. Monitor INR levels and adjust warfarin dose accordingly.
Fat malabsorption
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Use caution in all patients, especially with chronic bowel or pancreatic diseases. Initiate daily supplementation of vitamin E, linoleic acid, and omega-3 fatty acids.
Nausea, vomiting, dyspepsia
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Maintain a high level of suspicion, as lomitapide has been associated with an increased risk for these adverse events.
Specific populations
Renal impairment
eGFR ≥ 15 mL/min/1.73 m²
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Use acceptable. No dose adjustment required.
eGFR < 15 mL/min/1.73 m²
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Use with caution. Maximal dose of 40 mg per day.
Renal replacement therapy
Any modality
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Use with caution. Dose as in eGFR < 15 mL/min/1.73 m².
Hepatic impairment
Child-Pugh A (mild)
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Maximal dose of 40 mg per day. Monitor serum aminotransferases.
Child-Pugh B (moderate)
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Do not use.
Child-Pugh C (severe)
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Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters
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Do not use. Evidence of fetal harm in humans. Obtain a negative pregnancy test before initiating lomitapide and advise using reliable contraception while receiving treatment.
Breastfeeding
Do not use during breastfeeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
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Gastroenteritis, hepatic steatosis, ↑ liver enzymes, influenza virus infection, nasopharyngitis, abdominal pain, back pain, throat pain, chest pain, constipation, diarrhea, dyspepsia, fatigue, flatulence, abdominal distension, nausea, vomiting, weight loss
Common 1-10%
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Gastroesophageal reflux disease, angina pectoris, dizziness, fever, headache, nasal congestion, palpitations, tenesmus
Unknown frequency
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Fat malabsorption, hair loss, myalgia
Interactions
Drug(s)
Check Interactions
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