PCSK9 inhibitors - mechanisms of action.

PCSK9 is a proprotein convertase which is involved in the degradation of low-density lipoprotein (LDL) receptors in the liver. Mutations in the PCSK9 gene cause familial hypercholesterolaemia in a subset of patients by reducing the number of LDL receptors on the surface of hepatocytes. This decreases their ability to clear LDL cholesterol from plasma. Conversely, other PCSK9 mutations result in unusually low concentrations of plasma LDL cholesterol and a reduced risk of atherosclerotic disease. Blocking the activity of PCSK9 with monoclonal antibodies reduces the degradation of LDL receptors and increases the clearance of LDL cholesterol. An injection of PCSK9-specific antibody suppresses LDL-cholesterol concentrations for several weeks. [ABSTRACT FROM AUTHOR]

Copyright of Australian Prescriber is the property of Therapeutic Guidelines Limited and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)