Evolocumab is a human monoclonal antibody from the group of PCSK9 inhibitors. It is used to treat hypercholesterolemia.
Alirocumab is a drug from the group of PCSK9 inhibitors that are used to treat hypercholesterolemia.
PCSK9 inhibitors are monoclonal antibodies. Monoclonal antibodies are antibodies produced by a cell line ("cell clone") derived from a single B lymphocyte. They are directed against a specific, single epitope. In this case, they target the serine protease PCSK9 enzyme.
The serine protease PCSK9 has the function of binding to LDL receptors on the surface of liver cells (hepatocytes) and promoting their breakdown in the lysosomes. PCSK9 inhibitors selectively bind to circulating PCSK9 and inhibit their function. As a consequence, the enzyme can no longer bind to the LDL receptors.
As a result of the binding of the PCSK9 enzyme, the breakdown of the LDL receptors decreases.
Leading to an increase of LDL receptors on Hepatocytes.
The increased LDL receptors on the cell surface lead to a reduction in LDL cholesterol (LDL-C) in the blood, as it is increasingly absorbed by the liver cells.
PCSK9 inhibitors are used as second-line therapy in patients with hypercholesterolemia. Due to the current (2019) high costs, PCSK9 inhibitors are only used in familial hypercholesterolemia, therapy-refractory hypercholesterolemia with a very high cardiovascular risk, and when the standard therapy with statins plus ezetimibe has been exhausted and the LDL value is still above 140 mg/dl.
The drug is administered subcutaneously.
Skin Reaction at the Injection side is a common side effect of this drug.
Myalgia is a common side effect of this drug.
A common side effect of this drug is neurocognitive impairment.
Picmonic's rapid review multiple-choice quiz allows you to assess your knowledge.
*Average video play time: 2-3 minutes
Unforgettable characters with concise but impactful videos (2-4 min each)