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Effects of PCSK9 Inhibitors on Other than Low-Density Lipoprotein Cholesterol Lipid Variables

Theodosios D Filippatos1, Anastazia Kei1, Christos V Rizos1

  • 11 Department of Internal Medicine, School of Medicine, University of Ioannina, Ioannina, Greece.

Journal of Cardiovascular Pharmacology and Therapeutics
|August 23, 2017
PubMed

Insights

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors improve lipid profiles beyond lowering LDL-C. These drugs also benefit triglycerides, HDL-C, and Lp(a), potentially reducing cardiovascular risk.

Area of Science:

  • Cardiovascular Medicine
  • Lipid Metabolism
  • Pharmacology

Background:

  • Low-density lipoprotein cholesterol (LDL-C) is a primary cardiovascular risk factor.
  • Triglycerides (TRGs), high-density lipoprotein cholesterol (HDL-C), and lipoprotein a [Lp(a)] also significantly impact cardiovascular risk.
  • Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are potent LDL-C lowering agents.

Purpose of the Study:

  • To review the mechanisms behind PCSK9 inhibitors' effects on non-LDL-C lipid variables.
  • To explore how PCSK9 inhibition influences lipid and apolipoprotein metabolism.
  • To understand the broader impact of PCSK9 inhibitors on cardiovascular risk reduction.

Main Methods:

  • Literature review of studies on PCSK9 inhibitors and lipid metabolism.
  • Analysis of mechanisms affecting lipid and apolipoprotein secretion and clearance.
  • Investigation of effects on lipoprotein heteroexchange and related factors like sortilin.

Main Results:

  • PCSK9 inhibitors significantly reduce LDL-C.
  • These inhibitors also modestly improve TRGs and HDL-C concentrations.
  • PCSK9 inhibitors robustly decrease Lp(a) levels, suggesting broader lipid-modifying capabilities.

Conclusions:

  • PCSK9 inhibitors offer multifaceted benefits beyond LDL-C reduction.
  • The mechanisms involve modulation of lipid secretion, clearance, and inter-lipoprotein exchange.
  • PCSK9 inhibitors improve the overall lipid profile, contributing to cardiovascular risk reduction.

Keywords:
PCSK9 inhibitorsalirocumabevolocumabhigh-density lipoproteinlipoprotein aproprotein convertase subtilisin/kexin type 9triglycerides

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