PCSK9 inhibitors: current status and emerging frontiers in lipid control

Expert Rev Cardiovasc Ther. 2023 Nov 23. doi: 10.1080/14779072.2023.2288169. Online ahead of print.ABSTRACTINTRODUCTION: Atherosclerotic cardiovascular disease (ASCVD) is a leading cause of global mortality, imposing substantial healthcare economic burdens. Among the modifiable risk factors, hypercholesterolemia, especially elevated low-density lipoprotein cholesterol (LDL-C), plays a pivotal role in ASCVD development. Novel therapies such as PCSK9 (Proprotein Convertase Subtilisin/Kexin type 9) inhibitors are emerging to address this concern. These inhibitors offer the potential to reduce cardiovascular risk by directly targeting LDL-C levels.AREAS COVERED: The article delves into the structural and functional aspects of PCSK9, highlighting its role in LDL receptor regulation. The pharmacological strategies for PCSK9 inhibition, including monoclonal antibodies, binding peptides, gene silencing, and active immunization, are comprehensively explored. Clinical evidence from various trials underscores the safety and efficacy of PCSK9 inhibitors in reducing LDL-C levels and potentially improving cardiovascular outcomes. Despite the promising results, challenges such as cost-effectiveness and long-term safety considerations are addressed.EXPERT OPINION: Among PCSK9 inhibitors, monoclonal antibodies represent a cornerstone. Many trials have showed their efficacy in reducing LDL-C and the risk for major adverse clinical events, revealing prolonged effects, with special benefits part...
Source: Expert Review of Cardiovascular Therapy - Category: Cardiology Authors: Source Type: research