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 |