Evolocumab

Information about Evolocumab

Evolocumab is a human monoclonal antibody to PCSK9 (proprotein convertase subtilisin/kexin type 9), a circulating protein that modulates the activity of the LDL cholesterol receptor in the liver. The monoclonal antibody lowers serum LDL cholesterol and is used to treat severe hypercholesterolemia. Evolocumab therapy has been associated with a low rate of serum aminotransferase elevations and has yet to be linked to instances of clinically apparent acute liver injury.

Mechanism of action of Evolocumab

Evolocumab (e" voe lok' ue mab) is a human IgG1 monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9), a serine protease that decreases the activity of the LDL cholesterol receptor in the liver. Inhibition of PCSK9 increases the low density lipoprotein (LDL) cholesterol receptor, leading to an increased uptake of LDL particles and a decrease in serum LDL cholesterol. Patients with a genetic deficiency in PCSK9 have low levels of LDL cholesterol, and inhibition of the protein activity with monoclonal antibody leads to a marked lowering of LDL cholesterol. In several controlled trials, evolocumab was shown to lower LDL cholesterol in persons with heterozygosity for familial hypercholesterolemia and in persons at risk for atherosclerosis who have been unable to achieve adequate cholesterol lowering with standard lipid lowering agents (statins). Evolocumab

FDA approval information for Evolocumab

Evolocumab was approved for use in the United States in 2015. The current indications are limited to patients with severe hypercholesterolemia who are heterozygous for familial hypercholesterolemia or who have had clinical complications of atherosclerosis and an inadequate response to standard therapies. Evolocumab should be given in combination with advice on diet and exercise and in combination with oral lipid lowering agents such as statins.

Dosage and administration for Evolocumab

Evolocumab is available in solution in single use syringes or auto injectors of 140 mg/mL under the brand name Repatha.

Dosage and administration for Evolocumab

The recommended dose is 140 mg administered subcutaneously every 2 weeks or 420 mg (3 injections) every 4 weeks.

Side effects of Evolocumab

Side effects are not frequent and generally mild, and include injection site reactions, nasopharyngitis, upper respiratory tract infection, headache, myalgia and back pain. Rare, but potentially serious side effects may include hypersensitivity reactions and neurocognitive problems.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

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Medication resources

Learn more

• Dailymed label info
• Scientific articles

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