PCSK9 Inhibition: New Treatment Options and Perspectives to Lower Atherogenic Lipoprotein Particles and Cardiovascular Risk
Purpose of Review
To summarize latest clinical studies and to put them into perspectives for clinical relevant subgroups and new therapeutic options.
Have investigated PCSK9 inhibitors in patients with very high cardiovascular risk and insufficient LDL cholesterol lowering under current maximal tolerated lipid-lowering therapy, patients with statin intolerance, or genetic forms of familiar hypercholesterolemia, and patients on LDL apheresis. Purpose of recent cardiovascular endpoint trials has proven cardiovascular benefit of this new approach.
PCSK9 inhibition with fully humanized antibodies has proven to be effective, safe, and well-tolerated in reducing cardiovascular risk by LDL cholesterol lowering. Therefore, research interests are to elucidate additional roles and effects of PCSK9 modulation on inflammation and cellular processes of the atherosclerotic plaque and to develop alternative therapeutic strategies addressing PCSK9 as a proven and therefore promising drug target.
KeywordsPCSK9 Statin intolerance Familiar hypercholesterolemia LDL apheresis LDL receptor Atherosclerosis Hypercholesterolemia Non-HDL cholesterol
A key for cardiovascular risk reduction by lowering LDL cholesterol and load of atherogenic lipoproteins in serum is to increase the number of LDL receptors in the liver. This is a key mechanism of PCSK9 inhibitors. A clinical option is to use antibodies for the treatment of hypercholesterolemia preventing degradation of hepatic LDL receptors.
Compliance with Ethical Standards
Conflict of Interest
Julia Brandts declares no conflict of interest. Dirk Müller-Wieland has received speaker’s bureau and consultant/advisory board fees from Amgen, AstraZeneca, Boehringer Ingelheim, MSD (Merck), Novartis, Novo Nordisk, and Sanofi.
Human and Animal Rights and Informed Consent
This article does not contain any studies with human or animal subjects performed by any of the authors.
Papers of particular interest, published recently, have been highlighted as: • Of importance •• Of major importance
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