Summary of Pharmacology of PCSK9 and PCSK9 Inhibitors
| Target of action | PCSK9, a protein (protease) secreted primarily by liver, binds to LDL receptors on hepatocytes and promotes internalization and lysosomal degradation of LDL receptors, thereby reducing the number of LDL receptors. Reduction in LDL receptors result in elevated serum LDL-C levels. |
| Mechanism of action | PCSK9 inhibitors are monoclonal antibodies against PCSK9, thereby preventing internalization and lysosomal degradation of LDL receptors. This increases LDL receptor density, thereby reducing serum LDL-C levels. |
| Available products | Evolocumab and alirocumab are two commercially available PCSK9 inhibitors that are FDA approved for human use. |
| Mode of administration | Both evolocumab and alirocumab are administered as subcutaneous injection once a month or every 2 weeks |
| Storage | Should be stored in refrigerator and warmed to room temperature before use. |
PCSK9, proprotein convertase subtilisin/kexin type 9; LDL-C, low-density lipoprotein cholesterol; FDA, Federal Drug Administration.