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PCSK9 and Hypercholesterolemia: Therapeutic Approach

Milan Obradovic1, Bozidarka Zaric1, Emina Sudar-Milovanovic1

  • 1Institute of nuclear sciences Vinca, University of Belgrade, Laboratory of Radiobiology and Molecular Genetics, Belgrade, Serbia.

Current Drug Targets
|December 7, 2017
PubMed

Insights

New drugs targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) offer hope for hypercholesterolemia treatment. These PCSK9 inhibitors, including monoclonal antibodies and RNA interference, aim to reduce cardiovascular disease risk.

Area of Science:

  • Cardiovascular Medicine
  • Biochemistry
  • Pharmacology

Background:

  • Hypercholesterolemia and associated cardiovascular diseases are major global health concerns.
  • Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a critical role in regulating low-density lipoprotein receptor (LDLR) levels and serum LDL cholesterol.
  • Existing therapies for lipid disorders have limitations, driving the need for novel treatments.

Purpose of the Study:

  • To review recent findings on PCSK9's function, regulation, and its therapeutic potential.
  • To explore the development and limitations of current PCSK9 inhibitors.
  • To highlight PCSK9 as a therapeutic target for hypercholesterolemia and cardiovascular diseases.

Main Methods:

  • Review of basic and clinical studies on PCSK9.
  • Analysis of PCSK9 inhibitors, including monoclonal antibodies and RNA interference.
  • Evaluation of PCSK9's role in LDLR degradation and serum LDL levels.

Main Results:

  • PCSK9 inhibitors, such as monoclonal antibodies and RNA interference, have shown promise in managing hypercholesterolemia.
  • These inhibitors target PCSK9 to prevent LDLR degradation, thereby lowering serum LDL levels.
  • Cost-effectiveness remains a significant consideration for current PCSK9 inhibitor therapies.

Conclusions:

  • PCSK9 is a validated therapeutic target for hypercholesterolemia and related cardiovascular diseases.
  • Monoclonal antibodies and RNA interference represent key advancements in PCSK9 inhibition.
  • Further research is needed to address the cost-effectiveness and optimize the use of PCSK9 inhibitors in clinical practice.

Keywords:
PCSK9PCSK9 and CVDPCSK9 and hypercholesterolemiaPCSK9 therapyalirocumabevolocumab.

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