Evolocumab

Humanised monoclonal antibody and drug from the group of PCSK9 inhibitors (inhibitors).

Evolocumab acts as an inhibitor of the human enzyme PCSK9 (proprotein convertase subtilisin/exin type 9), which is involved in the regulation of cholesterol metabolism. The inhibitor is also approved if statins are not tolerated or are not sufficiently effective. The PCSK9 antibody can also be combined with statins or other lipid-lowering agents.

PCSK9 binds to the LDL receptor (LDL-R) and is taken up by liver cells in increased amounts. Binding to PCSK9 promotes endocytosis and degradation of the LDL receptor in endosomes. Thus, fewer LDL-receptors are available for recirculation to the cell surface. As a result, the binding of LDL cholesterol decreases. Evolocumab specifically binds serum PCSK9, thus preventing the formation of LDL-receptor-PCSK9 complexes and the intracellular degradation of the LDL receptor. Thus, increased LDL cholesterol can be absorbed by the LDL receptors and then degraded intracellularly.

Evolocumab is approved as a PCSK9 inhibitor in the EU for the reduction of cardiovascular risk (heart attack/stroke) for patients with hypercholesterolemia in secondary prevention.

Renata®

Evolocumab is the first PCSK9 inhibitor approved in the EU and is used for the treatment of familial hypercholesterolemia. The approval in the USA was granted in August 2015.