Evolution of LDL-C lowering medications and their cardiovascular benefits: Past, present, and future

Curr Probl Cardiol. 2024 Jul;49(7):102637. doi: 10.1016/j.cpcardiol.2024.102637. Epub 2024 May 10.

Abstract

Cardiovascular disease (CVD) is the leading cause of morbidity and mortality worldwide. Hyperlipidemia, particularly elevated low-density lipoprotein cholesterol (LDL-C) is one of the major risk factors for CVD. Major landmark cardiovascular outcome clinical trials demonstrated that LDL-C lowering medications reduce cardiovascular events, and the lower the LDL-C the better the outcome. This article discusses the evolution of LDL-C lowering medications starting from bile acid sequestrants (BAS), statin therapy, bempedoic acid, the proprotein convertase subtilisin kexin 9 (PCSK9) synthesis inhibitor, novel small interfering RNA-based therapy (inclisiran) to the most recent oral PCSK9 inhibitors (MK-0616) which is currently under phase 3 clinical trial studies.

Keywords: Cardiovascular benefits; Cholesterol medications; LDL-C lowering medications; LDL-C medications.

Publication types

  • Review

MeSH terms

  • Anticholesteremic Agents / therapeutic use
  • Cardiovascular Diseases* / drug therapy
  • Cardiovascular Diseases* / prevention & control
  • Cholesterol, LDL* / blood
  • Dicarboxylic Acids
  • Fatty Acids
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use
  • PCSK9 Inhibitors
  • RNA, Small Interfering

Substances

  • Cholesterol, LDL
  • Anticholesteremic Agents
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • PCSK9 Inhibitors
  • 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
  • ALN-PCS
  • Dicarboxylic Acids
  • Fatty Acids
  • RNA, Small Interfering