Generic Name and Formulations:
Lomitapide mesylate 5mg, 10mg, 20mg, 30mg, 40mg, 60mg; caps.
As an adjunct to low-fat diet and other lipid-lowering treatments, including LDL apheresis where available, to reduce LDL-C, total cholesterol, apo B, and non-HDL-C in patients with homozygous familial hypercholesterolemia (HoFH).
Not established in patients with hypercholesterolemia who do not have HoFH, including those with heterozygous familial hypercholesterolemia (HeFH). Effect on cardiovascular morbidity, mortality has not been determined.
Before starting: measure ALT, AST, alkaline phosphatase, total bilirubin; obtain (–) pregnancy test; initiate low-fat diet supplying <20% of energy from fat. Swallow whole. Take 2hrs after PM meal with water. Initially 5mg once daily. Titrate dose based on safety and tolerability: increase to 10mg daily after at least 2 weeks; and then at a minimum of 4-week intervals, to 20mg, 40mg, and up to max 60mg daily. Supplement with daily Vit.E, linoleic acid, ALA, EPA, and DHA. ESRD on dialysis, baseline mild hepatic impairment: max 40mg daily. Concomitant weak CYP3A4 inhibitors (eg, alprazolam, amiodarone, amlodipine, atorvastatin, bicalutamide, cilostazol, cimetidine, cyclosporine, fluoxetine, fluvoxamine, ginkgo, goldenseal, isoniazid, lapatinib, nilotinib, pazopanib, ranitidine, ranolazine, ticagrelor, zileuton): max 30mg daily; except oral contraceptives: max 40mg daily. Dose adjustments for elevated transaminases: see full labeling.
<18yrs: not established.
Pregnancy (Cat.X). Concomitant moderate (eg, amprenavir, aprepitant, atazanavir, ciprofloxacin, crizotinib, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, verapamil) or strong (eg, boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, mibefradil, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, tipranavir/ritonavir, voriconazole) CYP3A4 inhibitors. Moderate to severe hepatic impairment, active liver disease, unexplained persistent elevations of serum transaminases.
Elevations in transaminases and increases in hepatic fat may occur; measure ALT, AST, alkaline phosphatase, total bilirubin before initiating therapy, and then ALT, AST monthly or before any dose increase for 1st year; subsequently, at least every 3 months. Adjust dose if ALT or AST are ≥3xULN; discontinue if clinically significant liver injury, bilirubin ≥2xULN, or active liver disease occurs. Adhere to low-fat diet to reduce risk of GI effects. Galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption: avoid. Chronic bowel or pancreatic diseases that predispose to malabsorption. Renal impairment. Females of reproductive potential: use effective contraception. Nursing mothers: not recommended.
See Contraindications and Adults. Potentiated by CYP3A4 inhibitors (omit grapefruit juice). Potentiates warfarin; monitor INR. Risk of myopathy (including rhabdomyolysis) with simvastatin or lovastatin; reduce simvastatin dose by 50% (limit to 20mg daily [or 40mg daily for those previously tolerated simvastatin 80mg daily for ≥1 year without muscle toxicity]) or consider reducing lovastatin dose when initiating lomitapide. Consider dose reduction of P-gp substrates. Max one alcoholic drink/day. Caution with other hepatotoxic drugs (eg, isotretinoin, amiodarone, acetaminophen, methotrexate, tetracyclines, tamoxifen). Concomitant other LDL-lowering drugs: not recommended. Separate bile acid sequestrants by at least 4hrs.
Microsomal triglyceride transfer protein (MTP) inhibitor.
Diarrhea (if severe, consider reducing dose or suspending use), nausea, dyspepsia, vomiting, abdominal pain; hepatotoxicity (including steatohepatitis, hepatic failure) possible, reduced absorption of fat soluble vitamins.
Juxtapid REMS Program: only certified providers and pharmacies may prescribe and distribute.
Hepatic (CYP3A4; 1A2, 2B6, 2C8, 2C19 (minor); 99.8% protein bound.
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