Lipid lowering- alternative agents

Drug:  VASCEPA ® (icosapent ethyl) Capsules, for oral use
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ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval:  2012

Mechanism of Action:

INDICATIONS AND USAGE
VASCEPA is an ethyl ester of eicosapentaenoic acid (EPA) indicated as an adjunct to diet to reduce triglyceride (TG) levels in adult patients with severe (>/= 500 mg/dL) hypertriglyceridemia.

Limitations of Use:
The effect of VASCEPA on the risk for pancreatitis in patients with severe hypertriglyceridemia has not been determined.
The effect of VASCEPA on cardiovascular mortality and morbidity in patients with severe hypertriglyceridemia has not been determined.

DOSAGE AND ADMINISTRATION
The daily dose of VASCEPA is 4 grams per day taken as 2 capsules twice daily with food.

Patients should be advised to swallow VASCEPA capsules whole. Do not break open, crush, dissolve, or chew VASCEPA.

DOSAGE FORMS AND STRENGTHS
Capsules: 1 gram

CONTRAINDICATIONS:
VASCEPA is contraindicated in patients with known hypersensitivity (e.g., anaphylactic reaction) to VASCEPA or any of its components.

WARNINGS AND PRECAUTIONS
In patients with hepatic impairment, monitor ALT and AST levels periodically during therapy.

Use with caution in patients with known hypersensitivity to fish and/or shellfish.

ADVERSE REACTIONS
The most common reported adverse reaction (incidence >2% and greater than placebo) was arthralgia.

To report SUSPECTED ADVERSE REACTIONS, contact Amarin Pharma Inc. at 1-855-VASCEPA (1-855-827-2372) or contact the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS
Omega-3 acids may prolong bleeding time. Patients receiving treatment with VASCEPA and other drugs affecting coagulation (e.g., anti-platelet agents) should be monitored periodically.

Mechanism of Action: JUXTAPID directly binds and inhibits microsomal triglyceride transfer protein (MTP), which resides in the lumen of the endoplasmic reticulum, thereby preventing the assembly of apo B-containing lipoproteins in enterocytes and hepatocytes. This inhibits the synthesis of chylomicrons and VLDL. The inhibition of the synthesis of VLDL leads to reduced levels of plasma LDL-C.

INDICATIONS AND USAGE:  JUXTAPID is a microsomal triglyceride transfer protein inhibitor indicated as an adjunct to a low-fat diet and other lipid-lowering treatments, including LDL apheresis where available, to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with homozygous familial hypercholesterolemia (HoFH) (1).

Limitations of Use
The safety and effectiveness of JUXTAPID have not been established in patients with hypercholesterolemia who do not have HoFH (1).
The effect of JUXTAPID on cardiovascular morbidity and mortality has not been determined

DOSAGE AND ADMINISTRATION
Before treatment, measure ALT, AST, alkaline phosphatase, and total bilirubin; obtain a negative pregnancy test in females of reproductive potential; and initiate a low-fat diet supplying <20% of energy from fat (2.1).

Initiate treatment at 5 mg once daily. Titrate dose based on acceptable safety/tolerability: increase to 10 mg daily after at least 2 weeks; and then, at a minimum of 4-week intervals, to 20 mg, 40 mg, and up to the maximum recommended dose of 60 mg daily (2.1).

Due to reduced absorption of fat-soluble vitamins/fatty acids: Take daily vitamin E, linoleic acid, alpha-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA) supplements (2.1, 5.4).
Take once daily, whole, with water and without food, at least 2 hours after evening meal (2.2).

Patients with end-stage renal disease on dialysis or with baseline mild hepatic impairment should not exceed 40 mg daily (2.5, 2.6).

DOSAGE FORMS AND STRENGTHS
Capsules: 5 mg, 10 mg, 20 mg, 30 mg, 40 mg, and 60 mg (3).

CONTRAINDICATIONS:
Pregnancy.
Concomitant use with strong or moderate CYP3A4 inhibitors.
Moderate or severe hepatic impairment or active liver disease including unexplained persistent abnormal liver function tests.

Limitations of Use:
The safety and effectiveness of KYNAMRO have not been established in patients with hypercholesterolemia who do not have HoFH.
The effect of KYNAMRO on cardiovascular morbidity and mortality has not been determined.
The use of KYNAMRO as an adjunct to LDL apheresis is not recommended.

DOSAGE AND ADMINISTRATION
200 mg once weekly as a subcutaneous injection.
Before treatment, measure ALT, AST, alkaline phosphatase, and total bilirubin.

DOSAGE FORMS AND STRENGTHS
Single-use vial containing 1 mL of a 200 mg/mL solution
Single-use pre-filled syringe containing 1 mL of a 200 mg/mL solution

CONTRAINDICATIONS
Moderate or severe hepatic impairment, or active liver disease, including unexplained persistent elevations of serum transaminases.
Known sensitivity to product components.

WARNINGS AND PRECAUTIONS
Injection site reactions occur in 84% of patients and typically consist of one or more of the following: erythema, pain, tenderness, pruritus and local swelling.
Flu-like symptoms, which typically occur within 2 days after an injection, occur in 30% of patients and include one or more of the following: influenza-like illness, pyrexia, chills, myalgia, arthralgia, malaise or fatigue.