Juxtapid (lomitapide mesylate)

Dosage of lomitapide mesylate is expressed in terms of lomitapide.

The recommended initial adult dosage of lomitapide for management of homozygous familial hypercholesterolemia is 5 mg once daily; the initial dosage should be continued for at least 2 weeks. After 2 weeks (or longer), dosage may be increased gradually (i.e., at intervals of at least 4 weeks) in a stepwise manner (i.e., to 10, 20, 40, and then 60 mg once daily) based on safety and tolerability; liver function tests (or, at a minimum, ALT and AST concentrations) should be obtained prior to each dosage increase. The maintenance dosage of lomitapide should be individualized, taking into account the patient's goals and response to therapy; lomitapide dosage should not exceed 60 mg daily.

Lomitapide mesylate is administered orally once daily. To reduce the risk of adverse GI effects, the drug should be administered without food, at least 2 hours after the evening meal. Lomitapide capsules should be swallowed whole with a glass of water; capsules should not be opened, crushed, dissolved, or chewed.

If a dose of lomitapide is missed, the next dose should be taken at the regularly scheduled time. If therapy is interrupted for longer than 1 week, patients should contact their healthcare provider before reinitiating therapy.

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Lomitapide is metabolized in the liver principally by cytochrome P-450 (CYP) isoenzyme 3A4; the drug also may be metabolized to a small extent by CYP isoenzymes 1A2, 2B6, 2C8, and 2C19.

In vitro studies indicate that lomitapide inhibits CYP isoenzyme 3A4 but not CYP isoenzymes 1A2, 2B6, 2C9, 2C19, 2D6, or 2E1; the major metabolites of lomitapide, M1 and M3, do not inhibit CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4. In vitro studies indicate that lomitapide does not induce CYP isoenzymes 1A2, 3A4, or 2B6.

Lomitapide is not a substrate of P-glycoprotein (P-gp); however, the drug inhibits P-gp. Lomitapide does not inhibit the breast cancer resistance protein (BCRP).

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

Lomitapide mesylate is contraindicated in patients with moderate or severe hepatic impairment (Child-Pugh class B or C); patients with active liver disease, including unexplained, persistent elevations in serum aminotransferase concentrations; women who are pregnant; and patients receiving concomitant therapy with moderate or potent inhibitors of cytochrome P-450 (CYP) isoenzyme 3A4.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

Adverse effects reported in 10% or more of patients receiving lomitapide in the pivotal study include diarrhea, nausea, dyspepsia, vomiting, abdominal pain, weight loss, chest pain, abdominal discomfort, abdominal distention, constipation, flatulence, influenza, nasopharyngitis, increased ALT, fatigue, gastroenteritis, back pain, pharyngolaryngeal pain, gastroesophageal reflux disease, defecation urgency, rectal tenesmus, fever, headache, dizziness, nasal congestion, angina pectoris, and palpitations.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

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Safety and efficacy of lomitapide have not been established in pediatric patients.

Category X. (See Users Guide.) (See Cautions: Contraindications and also see Fetal/Neonatal Morbidity and Mortality under Warnings/Precautions: Other Warnings and Precautions, in Cautions.)

To monitor pregnancy outcomes in women who have been exposed to lomitapide, a pregnancy registry has been established. Clinicians are encouraged to enroll patients who become pregnant while receiving lomitapide in the registry; women also may enroll themselves in the registry by calling 877-902-4099 or visiting http://www.juxtapid.com.

It is not known whether lomitapide is distributed into human milk. Because many drugs are distributed into human milk and because of the potential for tumorigenicity (demonstrated in animal studies), a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Clinical studies of lomitapide did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger adults. Other reported clinical experience has not identified differences in responses between geriatric and younger patients. Dosage should be selected with caution. (See Dosage and Administration: Special Populations.)