Bococizumab (Pfizer) is an antidyslipidemic humanized antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protease involved in the intracellular and extracellular regulation of low-density lipoprotein receptor (LDLR) expression. It binds to the LDLR at the epidermal growth factor-like repeat A domain, targeting the receptor for lysosomal degradation within the hepatocytes. PCSK9 is also known to increase the production of apolipoprotein B-containing lipoproteins. Bococizumab inhibits the degradation of LDLR by preventing circulating PCSK9 from binding. This allows the receptors to be recycled to the surface of hepatocytes, leading to an increase in low-density lipoprotein cholesterol clearance.
Bococizumab (Pfizer) will likely be the third proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor to enter the dyslipidemia market. This third-to-market status may hinder bococizumab’s uptake as it will have to compete with Repatha (evolocumab; Amgen/Astellas) and Praluent (alirocumab; Sanofi/Regeneron) at launch. Additionally, cardiovascular (CV) outcomes data for both Repatha and Praluent are expected to be released before bococizumab, further decreasing the drug’s competitive potential within the PCSK9 inhibitor space. However, the broad patient base in Pfizer’s CV outcomes trial (CVOT) program may help demonstrate value to payers if bococizumab can demonstrate a reduction in CV risk in patients receiving a high-dose statin with uncontrolled low-density lipoprotein cholesterol (LDL-C) levels. Pfizer also intends to explore a once-monthly formulation of bococizumab that will utilize Halozyme’s Enhanze technology.
TABLE OF CONTENTS
4 PRODUCT PROFILES
4 bococizumab : Dyslipidemia
LIST OF FIGURES
12 Figure 1: Bococizumab for dyslipidemia – SWOT analysis
13 Figure 2: Datamonitor Healthcare’s drug assessment summary of bococizumab for
13 Figure 3: Datamonitor Healthcare’s drug assessment summary of bococizumab for
LIST OF TABLES
4 Table 1: Bococizumab drug profile
6 Table 2: Bococizumab Phase III data in dyslipidemia
8 Table 3: Bococizumab Phase III trials in dyslipidemia
11 Table 4: Bococizumab efficacy in adults with high cholesterol on statin therapy
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