Drug intelligence / Profile preview

tafolecimab

Development stage
Phase 4
Lead developer
Innovent Biologics Technology Limited (Shanghai R&D Center)
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Subcutaneous
01

Overview

Tafolecimab is a fully human IgG2κ monoclonal antibody that targets proprotein convertase subtilisin/kexin type 9 (PCSK9). By binding to PCSK9, tafolecimab prevents its interaction with the low-density lipoprotein receptor (LDLR), thereby restoring LDLR recycling and increasing LDL cholesterol uptake by the liver. This results in significant reductions in circulating LDL cholesterol levels as well as total cholesterol and apolipoprotein B. Tafolecimab is administered subcutaneously and has demonstrated efficacy in reducing LDL-C by approximately 70% in clinical trials. It was developed by Innovent for the treatment of primary hyperlipidemia—including heterozygous familial hypercholesterolemia (HeFH) and non-familial forms—and mixed dyslipidemia, particularly for patients who have not achieved target lipid levels despite statin therapy. The drug received its first approval in China in August 2023[1][3][6][8].

Brand names
SINTBILO
Other names
Immunoglobulin igg2, anti-(human proprotein convertase subtilisin/kexin type 9) (human monoclonal ibi306 .gamma.2-chain), disulfide with human monoclonal ibi306 .kappa.-chain, dimer
02

Targets

PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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