Generic Name and Formulations:
Lomitapide mesylate 5mg, 10mg, 20mg; caps.

Company:
Aegerion Pharmaceuticals
   

Indications for JUXTAPID:

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). Limitations of use: not for patients with hypercholesterolemia who do not have HoFH. Effect on cardiovascular morbidity, mortality has not been determined.

Adult Dose for JUXTAPID:

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. 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 or 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, oral contraceptives, pazopanib, ranitidine, ranolazine, tipranavir/ritonavir, ticagrelor, zileuton): max 30mg daily. Dose adjustments for elevated transaminases: see full labeling.

Children's Dose for JUXTAPID:

<18yrs: not established.

Pharmacological Class:

Microsomal triglyceride transfer protein (MTP) inhibitor.

Rems:

YES

Contraindications:

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, voriconazole) CYP3A4 inhibitors. Moderate to severe hepatic impairment, active liver disease, unexplained persistent elevations of serum transaminases.

Warnings/Precautions:

Elevations in transaminases and increases in hepatic fat may occur; measure ALT, AST, alkaline phosphatase, total bilirubin before initiating therapy and then ALT, AST regularly and before any dose increase. Adjust dose if ALT or AST are ≥3xULN; discontinue if clinically significant liver toxicity. 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: use effective contraception. Nursing mothers: do not use.

Interactions:

See Contraindications and Adults. Potentiated by CYP3A4 inhibitors (omit grapefruit juice). Reduce dose of simvastatin by 50%, consider reducing lovastatin dose. Potentiates warfarin; monitor INR. Consider dose reduction of P-gp substrates. Max one alcoholic drink/day. Caution with other hepatotoxic drugs. Separate bile acid sequestrants by at least 4hrs.

Adverse Reactions:

GI upset, dyspepsia, abdominal pain; hepatotoxicity (including steatohepatitis, hepatic failure) possible, reduced absorption of fat soluble vitamins.

Note:

Juxtapid REMS Program: only certified providers and pharmacies may prescribe and distribute.

Metabolism:

Hepatic (CYP3A4; 1A2, 2B6, 2C8, 2C19 (minor); 99.8% protein bound.

Elimination:

Renal, fecal.

Generic Availability:

NO

How Supplied:

Caps—28
Juxtapid ( 甲磺酸洛美他派胶囊)
Aegerion's公司研制开发的洛美他派(lomitapide)甲磺酸盐于2012年12月21日由美国FDA批准在美国上市,商品名为Juxtapid。该药为胶囊剂,用于治疗纯合子家族性高胆固醇血症(HoFH)。该药获准与低脂饮食和其他降脂药物一起使用治疗HoFH,可降低患者的低密度脂蛋白胆固醇、总胆固醇、载脂蛋白B和非高密度脂蛋白胆固醇[1]。洛美他派甲磺酸盐的中文化学名称:N-(2,2,2-三氟乙基)-9-{4-{4-[4'-(三氟甲基)[1,1'-联苯基]-2-甲酰胺基]哌啶-1-基}丁基}-9H-芴基-9-甲酰胺甲磺酸盐;英文化学名称:N-(2,2,2-trifluoroethyl)-9-{4-{4-[4'-(trif-luoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl}butyl}-9H-fluorene-9-carboxamide mesylate;分子式:C39H37F6N3O2;分子量:789.8;CAS登记号:182431-12-5

Indication and Important Safety Information

JUXTAPID is used along with a low-fat diet and other lipid-lowering treatments, including LDL apheresis where available, in people with HoFH. It is not known whether JUXTAPID can decrease problems from high cholesterol, such as heart attack, stroke, death or other health problems. It is also not known whether Juxtapid is safe for use in people with high cholesterol but who do not have HoFH. 

IMPORTANT SAFETY INFORMATION
JUXTAPID can cause serious side effects, including liver problems. For this reason, your doctor should do blood tests to check your liver before you start JUXTAPID, if your dose is increased, and while you take JUXTAPID. If your tests show some liver problems, your doctor may adjust your dose of JUXTAPID or stop it altogether.

You should tell your doctor if you have had liver problems, including liver problems while taking other medicines.

JUXTAPID is available only through certified pharmacies that are enrolled in the JUXTAPID REMS Program. Your doctor must be enrolled and certified in the program in order for you to be prescribed JUXTAPID.

You should not take JUXTAPID if:

• You are pregnant
• You are taking medications known as moderate or strong CYP3A4 inhibitors, which affect how the body breaks down JUXTAPID
• You have moderate or severe liver problems or active liver disease, including elevated liver function tests

JUXTAPID may cause harm to your unborn baby. If you are pregnant, think you may be pregnant, or are planning to become pregnant, do not take JUXTAPID. Do not have sex while taking JUXTAPID unless you are using effective birth control. If you become pregnant while taking JUXTAPID, stop taking JUXTAPID and call your doctor right away.

Diarrhea, nausea/vomiting, and stomach pain/discomfort are very common with JUXTAPID. Strictly following a low-fat diet may help lower the chance of having these symptoms. These side effects can also be symptoms of liver problems. Tell your doctor right away if you have any of these symptoms of liver problems while taking JUXTAPID:  nausea; vomiting or stomach pain that gets worse, does not go away, or changes; fever; yellowing of your eyes or skin; feeling more tired than usual; having flu-like symptoms.

JUXTAPID makes it harder for some nutrients to get into your body. Take Vitamin E and fatty acids each day while you take JUXTAPID. Ask your doctor, nurse, or dietician how to add them to your diet.

The most common side effects of JUXTAPID include diarrhea (loose stool), 
nausea, vomiting, stomach cramping or pain, indigestion, and gas. Tell your doctor if you have any side effect that bothers you or that does not go away.
These are not all the possible side effects of JUXTAPID. For more information, ask your doctor or pharmacist.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. JUXTAPID may affect the way other medicines work, and other medicines may affect how JUXTAPID works. You should not drink grapefruit juice while taking JUXTAPID.

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088.

http://www.juxtapid.com/