A Review of PCSK9 Inhibitors and their effects on cardiovascular disease

• Published in: Current topics in medicinal chemistry
• Main Authors: Chen, Bo, Zhao, Pengjun, Shi, Xin, Cui, Yanping, Hou, Aiping
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 08.08.2019
• Subjects: hypercholesterolemiProprotein convertase subtilisin/kexin type 9 (PCSK9); inhibitors; clinical effect; Proprotein convertase subtilisin/kexin type 9 (PCSK9); pharmacokinetic; hypercholesterolemia; pharmacodynamic profile

Cardiovascular disease remains the leading cause of morbidity and mortality in the world, with elevated low density lipoprotein-cholesterol (LDL-C) levels as a major risk factor. Lower levels of LDL-C can effectively reduce the risk of cardiovascular disease. Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in regulating the degradation of hepatic LDL receptors that remove LDL-C from the circulation. PCSK9 inhibitors are a new class of agents that are becoming increasingly important as treatments to reduce LDL-C levels. Two PCSK9 inhibitors, alirocumab and evolocumab, have been approved to treat hypercholesterolemia and are available in the United States and European Union. Through inhibition of PCSK9 and increased recycling of LDL receptors, they can significantly reduce serum LDL-C levels. This review will describe the chemistry, pharmacokinetics, and pharmacodynamics of PCSK9 inhibitors and their clinical effects.