Drug intelligence / Profile preview

bococizumab + atorvastatin

Development stage
Phase 2
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

Bococizumab + atorvastatin is a combination therapy studied for the treatment of primary hypercholesterolemia and prevention of cardiovascular events. Bococizumab is a humanized IgG2Δa monoclonal antibody that targets proprotein convertase subtilisin/kexin type 9 (PCSK9), reducing low-density lipoprotein cholesterol (LDL-C) by increasing hepatic clearance of LDL via LDL receptor upregulation. Atorvastatin is a small molecule HMG-CoA reductase inhibitor (statin) that decreases cholesterol synthesis in the liver and upregulates LDL receptor expression. Bococizumab was developed by Pfizer, and clinical studies demonstrated that when combined with atorvastatin, LDL-C levels were substantially reduced compared to atorvastatin alone. However, bococizumab was discontinued in development due to attenuation of LDL reduction over time and immunogenicity concerns. The combination is not approved for clinical use but was studied up to phase 3 in high-risk cardiovascular populations[1][2][3][5][6].

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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