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RISK OF HEPATOTOXICITY
JUXTAPID can cause elevations in transaminases. In the JUXTAPID clinical trial, 10 (34%) of the 29 patients treated with JUXTAPID had at least one elevation in alanine aminotransferase (ALT) or aspartate aminotransferase (AST) ≥ 3x upper limit of normal (ULN). There were no concomitant clinically meaningful elevations of total bilirubin, international normalized ratio (INR), or alkaline phosphatase [see WARNINGS AND PRECAUTIONS].
JUXTAPID also increases hepatic fat, with or without concomitant increases in transaminases. The median absolute increase in hepatic fat was 6% after both 26 and 78 weeks of treatment, from 1% at baseline, measured by magnetic resonance spectroscopy. Hepatic steatosis associated with JUXTAPID treatment may be a risk factor for progressive liver disease, including steatohepatitis and cirrhosis [see WARNINGS AND PRECAUTIONS].
Measure ALT, AST, alkaline phosphatase, and total bilirubin before initiating treatment and then ALT and AST regularly as recommended. During treatment, adjust the dose of JUXTAPID if the ALT or AST are ≥ 3x ULN. Discontinue JUXTAPID for clinically significant liver toxicity [see DOSAGE AND ADMINISTRATION and WARNINGS AND PRECAUTIONS].
Because of the risk of hepatotoxicity, JUXTAPID is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the JUXTAPID REMS PROGRAM [see WARNINGS AND PRECAUTIONS].
JUXTAPID capsules contain lomitapide mesylate, a synthetic lipid-lowering agent for oral administration.
The chemical name of lomitapide mesylate is N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4'(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9carboxamide, methanesulfonate salt. Its structural formula is:
The empirical formula for lomitapide mesylate is C39H37F6N3O2 • CH4O3S and its molecular weight is 789.8.
Lomitapide mesylate is a white to off-white powder that is slightly soluble in aqueous solutions of pH 2 to 5. Lomitapide mesylate is freely soluble in acetone, ethanol, and methanol; soluble in 2-butanol, methylene chloride, and acetonitrile; sparingly soluble in 1-octanol and 2-propanol; slightly soluble in ethyl acetate; and insoluble in heptane.
Each JUXTAPID capsule contains lomitapide mesylate equivalent to 5, 10, or 20 mg lomitapide free base and the following inactive ingredients: pregelatinized starch, sodium starch glycolate, microcrystalline cellulose, lactose monohydrate, silicon dioxide and magnesium stearate. The capsule shells contain gelatin and titanium dioxide. In addition, the orange capsule shells contain red iron oxide. The imprinting ink contains shellac, black iron oxide, and propylene glycol.
Last reviewed on RxList: 2/27/2014
This monograph has been modified to include the generic and brand name in many instances.
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