Repatha Vs. Zetia: Drug Comparison

Repatha^® (evolocumab) is a monoclonal antibody that lowers LDL cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9), which enhances the liver's ability to remove LDL cholesterol from the blood. Its FDA-approved indications include use in adults with established cardiovascular disease to reduce the risk of heart attack, stroke, and coronary revascularization. It is also approved as an adjunct to diet, alone or in combination with other LDL-cholesterol-lowering therapies, for adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH), to reduce LDL cholesterol. Additionally, Repatha is indicated as an adjunct to diet and other LDL-cholesterol-lowering therapies in pediatric patients aged 10 years and older with HeFH, and for both adults and pediatric patients aged 10 years and older with homozygous familial hypercholesterolemia (HoFH), to reduce LDL cholesterol levels. Repatha is administered as a subcutaneous injection, typically once or twice a month. Common side effects include injection site reactions, cold-like symptoms, and muscle pain. Caution is advised for patients with hypersensitivity to monoclonal antibodies.

Zetia^® (ezetimibe) is a cholesterol-lowering medication that works by inhibiting the absorption of cholesterol in the small intestine, which reduces the amount of cholesterol delivered to the liver and helps lower LDL cholesterol levels in the blood. Its FDA-approved indications include the treatment of primary hyperlipidemia, either alone or in combination with statins, and the treatment of homozygous familial hypercholesterolemia and sitosterolemia. Zetia is available in tablet form and is typically taken once daily. Common side effects include upper respiratory infection, headache, diarrhea, and fatigue, while serious risks are rare but may include liver enzyme elevations when combined with statins. Zetia should be used with caution in patients with moderate to severe liver impairment.

Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor

Selective cholesterol-absorption inhibitor

Repatha (evolocumab) is indicated:

• In adults with established cardiovascular disease (CVD) to reduce the risk of myocardial infarction, stroke, and coronary revascularization

• As an adjunct to diet, alone or in combination with other low-density lipoprotein cholesterol (LDL-C)-lowering therapies, in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH), to reduce LDL-C

• As an adjunct to diet and other LDL-C-lowering therapies in pediatric patients aged 10 years and older with HeFH, to reduce LDL-C

• As an adjunct to other LDL-C-lowering therapies in adults and pediatric patients aged 10 years and older with homozygous familial hypercholesterolemia (HoFH), to reduce LDL-C

Zetia (ezetimibe) is indicated:

• In combination with a statin, or alone when additional low density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH)

• In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH

• In combination with fenofibrate as an adjunct to diet to reduce elevated LDL-C in adults with mixed hyperlipidemia

• In combination with a statin, and other LDL-C lowering therapies, to reduce elevated LDL-C levels in adults and in pediatric patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH)

• As an adjunct to diet for the reduction of elevated sitosterol and campesterol levels in adults and in pediatric patients 9 years of age and older with homozygous familial sitosterolemia

• Typically taken as an injection every two weeks or monthly

• Comes in 140 mg/mL solution single-dose syringes and autoinjectors and as 420 mg/3.5 mLsolution on-body infusor system

• Typically taken once daily

• Comes in 10 mg tablets

Common (>5% of patients treated with Repatha and more frequently than placebo) adverse reactions in adults with:

Primary hyperlipidemia:

• Nose and throat inflammation

• Upper respiratory tract infection

• Influenza

• Back pain

• Injection site reactions

Established CVD:

• Diabetes mellitus

• Nose and throat inflammation

• Upper respiratory tract infection

Common adverse reactions in clinical trials:

Zetia administered alone (incidence ≥2% and greater than placebo):

• Upper respiratory tract infection

• Diarrhea

• Joint pain

• Inflammation of the sinuses

• Pain in extremity

• Fatigue

• Influenza

Zetia coadministered with a statin (incidence ≥2% and greater than statin alone):

• Inflammation of the nasal passages and throat

• Muscle pain

• Upper respiratory tract infection

• Joint pain

• Diarrhea

• Back pain

• Influenza

• Pain in extremity

• Fatigue

• Patients with a history of a serious hypersensitivity reaction to evolocumab or any of the excipients in Repatha

• Hypersensitivity to ezetimibe or any excipient of Zetia

• When used in combination with a statin, fenofibrate, or other LDL-C lowering therapy, Zetia is contraindicated in patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated. Refer to the Full Prescribing Information of these products for a list of their contraindications

• Drug interactions: Cyclosporine, fibrates, bile acid sequestrants

• Hypersensitivity reactions: Angioedema has occurred

• Risks associated with combination treatment with a statin, fenofibrate, or other LDL-C lowering therapies

• Liver enzyme abnormalities and monitoring

• Skeletal muscle effects (e.g., myopathy and rhabdomyolysis)

*This information is from the label for brand name Repatha^®. See the Full Prescribing Information for more complete information.

*This information is from the label for brand name Zetia. See the Full Prescribing Information for more complete information. Ezetimibe, the active ingredient in Zetia, may also be the active ingredient in other medications, and this information may not be accurate for all medications that include the active ingredient ezetimibe.