Alirocumab: PCSK9 inhibitor for LDL cholesterol reduction

Hagai Tavori, Michelle Melone, Shirya Rashid

Research output: Contribution to journalReview articlepeer-review

14 Scopus citations


The proof of concept that proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition affects cholesterol levels was first established after the demonstration that PCSK9 loss-of-function mutations result in a significant drop in circulating LDL cholesterol levels. Subsequent studies revealed that PCSK9 binds the epidermal growth factor precursor homology domain-A on the surface LDL Receptor (LDLR) and directs LDLR and PCSK9 for lysosomal degradation. Alirocumab (also known as SAR236553/REGN727) is a monoclonal antibody that binds circulating PCSK9 and blocks its interactions with surface LDLR. Alirocumab clinical trials with different doses on different administration schedules were shown to significantly reduce LDL cholesterol both as a mono-therapy and in combination with statins or ezetimibe. Although there is great potential for anti-PCSK9 therapies in the management of cholesterol metabolism, there is no clear evidence yet that blocking PCSK9 reduces cardiovascular disease outcome. This is being investigated in ongoing Phase III clinical trials with alirocumab.

Original languageEnglish (US)
Pages (from-to)1137-1144
Number of pages8
JournalExpert Review of Cardiovascular Therapy
Issue number10
StatePublished - Oct 1 2014
Externally publishedYes


  • Familial hypercholesterolemia
  • Low-density lipoprotein
  • Low-density lipoprotein receptor
  • Monoclonal antibodies
  • PCSK9

ASJC Scopus subject areas

  • Internal Medicine
  • Cardiology and Cardiovascular Medicine


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