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LDL cholesterol-lowering therapies: emphasis on proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors

F Sabatel-Pérez1, A García-Ropero2, C G Santos-Gallego2

  • 1Atherothrombosis Research Unit, Mount Sinai Heart, Icahn School of Medicine at Mount Sinai, New York, New York, USA; Cardiology Deparment, Complejo Hospitalario de Toledo, Toledo, Spain.

Drugs of Today (Barcelona, Spain : 1998)
|May 28, 2019
PubMed

Insights

Lowering low-density lipoprotein cholesterol (LDL-C) is crucial for managing atherosclerotic cardiovascular disease. Newer therapies like PCSK9 inhibitors offer improved control, supporting the

Area of Science:

  • Cardiology
  • Metabolic Disorders
  • Pharmacology

Background:

  • Atherosclerotic cardiovascular disease (ASCVD) is a primary global cause of mortality.
  • Hypercholesterolemia, particularly elevated low-density lipoprotein cholesterol (LDL-C), is a significant risk factor for ASCVD.
  • Established clinical trials confirm a strong correlation between LDL-C levels and cardiovascular events.

Purpose of the Study:

  • To review the development and efficacy of lipid-lowering therapies for managing hypercholesterolemia.
  • To highlight the role of newer agents like ezetimibe and PCSK9 inhibitors in achieving target LDL-C levels.
  • To reinforce the 'lower is better' and 'earlier is better' principles in ASCVD management.

Main Methods:

  • Literature review of clinical trials and pharmacological data.
  • Analysis of the cholesterol biosynthesis and metabolism pathways.
  • Evaluation of the effectiveness of statins, ezetimibe, and PCSK9 inhibitors.

Main Results:

  • Statins are foundational but may not achieve target LDL-C reduction alone.
  • Ezetimibe and PCSK9 inhibitors represent more potent therapeutic options.
  • Recent studies support aggressive LDL-C lowering for better cardiovascular outcomes.

Conclusions:

  • The 'lower the better' principle is reinforced by advanced lipid-lowering therapies.
  • Early intervention in atherosclerotic pathophysiology is critical for improved prognosis.
  • PCSK9 inhibitors and ezetimibe offer significant advancements in managing hypercholesterolemia and reducing cardiovascular risk.

Keywords:
HypercholesterolemiaLDL cholesterolLipoprotein disordersMetabolic diseasesPCSK9 inhibitorsStatins

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