Introduction of Bococizumab

Bococizumab is a monoclonal antibody that was development by Pfizer targeting proprotein convertase subtilisin kexin type 9 (PCSK9). Pfizer withdrew the drug from development in November 2016, because after six phase III clinical trials, bococizumab was found to be more immunogenic compared to evolocumab and alirocumab, and more serious is the gradual decline in efficacy due to the production of neutralizing antibodies.

Mechanism of Action of Bococizumab

PCSK9 is an enzyme secreted by the liver and typically binds to the low-density lipoprotein (LDL) receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL cholesterol (LDL-C) and therefore reducing the clearance of LDL-C from plasma. Therefore, bococizumab inhibits PCSK9's actions and allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance.

Fig.1 Mechanism of action of bococizumab

For research use only. Not intended for any clinical use.