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A Familial Hypercholesterolemia Human Liver Chimeric Mouse Model Using Induced Pluripotent Stem Cell-derived Hepatocytes
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Emerging biologic therapies for hypercholesterolaemia

Giacomo Pucci1,2, Arrigo F Cicero3, Claudio Borghi3

  • 1a Dipartimento di Medicina , Università di Perugia , Perugia , Italy.

Expert Opinion on Biological Therapy
|June 16, 2017
PubMed

Insights

Monoclonal antibodies targeting PCSK9 effectively lower LDL-cholesterol, reducing cardiovascular disease risk. Further LDL-C reduction with PCSK9 inhibition offers enhanced protection for high-risk individuals.

Area of Science:

  • Cardiology
  • Pharmacology
  • Biochemistry

Background:

  • Low-density lipoprotein cholesterol (LDL-C) is a primary risk factor for cardiovascular disease (CV).
  • Therapies reducing LDL-C are proven effective in mitigating atherosclerotic CV disease risk.
  • Monoclonal antibodies (mAbs) targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) represent a novel therapeutic approach.

Purpose of the Study:

  • To review the efficacy of PCSK9-targeting mAbs in reducing LDL-C and other atherogenic lipids.
  • To discuss the implications of bococizumab's discontinuation and inclisiran's development.
  • To evaluate the role of PCSK9 inhibition in enhancing cardiovascular protection.

Main Methods:

  • Review of current literature on PCSK9 inhibitors.
  • Analysis of clinical trial data for PCSK9 monoclonal antibodies and inclisiran.
  • Discussion of cardiovascular outcomes and safety profiles.

Main Results:

  • PCSK9 inhibition effectively lowers LDL-C and other atherogenic lipid fractions.
  • Bococizumab development was halted due to safety and efficacy issues.
  • Inclisiran shows promise as a long-acting PCSK9 inhibitor.
  • Early data suggest additional CV protection with PCSK9 inhibition alongside standard therapies in high-risk patients.

Conclusions:

  • PCSK9 inhibition, particularly with mAbs, offers a significant advancement in LDL-C reduction strategies.
  • Further LDL-C lowering via PCSK9 inhibition may provide additional cardiovascular protection for high-risk populations.
  • These therapies have the potential to reshape cardiovascular risk management, though cost-effectiveness requires further evaluation.
Abstract

Keywords:
HypercholesterolemiaLDL cholesterolPCSK9alirocumabbiologic therapycardiovascular diseasecardiovascular riskdyslipidemiaevolocumablipoproteinsproprotein convertase subtilisin/kexin type 9 inhibitors

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