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. 2021 Oct 15;8:764038. doi: 10.3389/fcvm.2021.764038

Table 1.

PSCK9 inhibitors.

Name Strategy Target Mechanism Status
Evolocumab Humanized monoclonal antibody CAT of PCSK9 Blocking PCSK9 binding to LDLR Approved
Alirocumab Humanized monoclonal antibody CAT of PCSK9 Blocking PCSK9 binding to LDLR Approved
Inclisiran GalNAc-conjugated siRNA mRNA of PCSK9 Inhibiting PCSK9 expression Under review by the FDA
LIB003 Adnectin-human serum albumin fusion protein CAT of PCSK9 Blocking PCSK9 binding to LDLR Phase III
AT04A and AT06A PCSK9 peptide Vaccine Aa 153-162 of PCSK9 Blocking PCSK9 binding to LDLR Phase I
Mimetic peptide Mimicking the binding site of PCSCK9 on LDLR CAT of PCSK9 Blocking PCSK9 binding to LDLR Preclinical
DRP Small PCSK9 inhibitor Inhibiting interaction between PCSK9 and HSPG Preclinical
NYX-330 Small PCSK9 inhibitor PCSK9 Inhibition of PCSK9 binding to LDLR Preclinical
PF-0644846 Inhibitor of ribosome 80S ribosome Inhibition of PCSK9 translation Preclinical
CRISPR-Cas9 Gene editing PCSK9 gene Knockout/knockdown of PCSK9 expression Preclinical
9k Small inhibitor, berberine derivative The HNF1α pathway Inhibition of PCSK9 transcription Preclinical
7030B-C5 Small inhibitor the FoxO1 and HNF1α pathway Inhibition of PCSK9 transcription Preclinical