Drug intelligence / Profile preview

bococizumab + statin

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

Overview

A combination therapy consisting of **bococizumab**, a humanized monoclonal antibody developed to inhibit **proprotein convertase subtilisin/kexin type 9 (PCSK9)**, and a **statin** (standard-of-care HMG-CoA reductase inhibitor). Bococizumab binds to and inhibits PCSK9, prolonging the half-life of hepatic low-density lipoprotein (LDL) receptors and thereby increasing hepatic clearance of LDL cholesterol. Statins lower cholesterol primarily by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. The combination was studied for its potential to further reduce LDL-C and cardiovascular risk in statin-treated patients with hypercholesterolemia or high cardiovascular risk, especially those with persistently high LDL despite statin therapy. Bococizumab development was discontinued after phase 3 trials due to attenuation of LDL lowering over time and variable individual efficacy, largely attributed to the development of anti-drug antibodies. Statins remain the cornerstone of therapy in dyslipidemia management.

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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