Table 1.
Therapeutic Approaches Targeting PCSK9. Adapted from Urban et al. Targeting the Proprotein Convertase Subtilisin/Kexin Type 9 for the Treatment of Dyslipidemia and Atherosclerosis. J Am Coll Cardiol 2013;62:1401–8.13
| Mechanism of Action | Agent | Company/Sponsor | Phase |
| Monoclonal antibodies | SAR236553/REGN727 | Sanofi/Regeneron | 3 |
| AMG 145 | Amgen | 3 | |
| RN316 | Pfizer | 2 | |
| RG7652 | Roche/Genentech | 2 | |
| LGT-209 | Novartis | 2 | |
| 1D05-lgG2 | Merck | Pre-clinical | |
| 1B20 | Merck | Pre-clinical | |
| J10, J16 | Pfizer | Pre-clinical | |
| J17 | Pfizer | Pre-clinical | |
| Adnectins | BMS-962476 | Bristol-Myers Squibb/Adnexus | 1 |
| Mimetic peptides | EGF-AB peptide fragment | Schering-Plough | Pre-clinical |
| LDLR (H306Y) subfragment | US NIH | Pre-clinical | |
| LDLR DNA construct | US NIH | Pre-clinical | |
| Small molecule inhibitors | SX-PCK9 | Serometrix | Pre-clinical |
| TBD | Shifa Biomedical | Pre-clinical | |
| Antisense oligonucleotides | ISIS 394814 | Isis | Pre-clinical |
| SPC4061 | Santaris-Pharma | Pre-clinical | |
| SPC5011 | Santaris-Pharma | 1 (terminated) | |
| RNA interference | ALN-PCS02 | Alnylam | 1 |