"The U.S. Food and Drug Administration today approved Kynamro (mipomersen sodium) injection as an addition to lipid-lowering medications and diet to treat patients with a rare type of high cholesterol called homozygous familial hypercholesterolemi"...
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 normalize d 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 bas eline, 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 live r 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 (REM S) called the JUXTAPID REMS Program [see WARNINGS AND PRECAUTIONS]. Prescribe JUXTAPID only to patients with a clinical or laboratory diagnosis consistent with HoFH. The safety and effectiveness of JUXTAPID have not been established in patients with hyperchole sterolemia who do not have HoFH [see INDICATIONS AND USAGE].
JUXTAPID capsules contain lomitapide mesylate, a synthetic lipid-lowering agent for oral administration.
The chemical name of lomitapide mesylate is N-(2,2,2-trifluor oethyl)-9-[4-[4-[[[ 4'(trifluoromethy l)[1,1'-biphenyl]-2-yl]carbonyl]a mino]-1-piper idinyl]but yl]-9H-f luorene-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, 20, 30, 40 or 60 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 of all strengths contain gelatin and titanium dioxide; the 5 mg, 10 mg and 30 mg capsules also contain red iron oxide; and the 30 mg, 40 mg and 60 mg capsules also contain yellow iron oxide. The imprinting ink contains shellac, black iron oxide, and propylene glycol.
What are the possible side effects of lomitapide (Juxtapid)?
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Stop using lomitapide and call your doctor at once if you have signs of a liver problem, such as:
- nausea, upper stomach pain, loss of appetite;
- dark urine, clay-colored stools; or
- itching, or jaundice (yellowing of the skin or eyes).
Common side effects may include:
- vomiting, gas, indigestion, stomach pain;
- diarrhea, constipation;
- chest pain;...
Last reviewed on RxList: 5/31/2016
This monograph has been modified to include the generic and brand name in many instances.
Additional Juxtapid Information
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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