Tafolecimab (IBI-306): A Comprehensive Monograph on a Novel, Long-Acting PCSK9 Inhibitor for Hypercholesterolemia

Executive Summary

Tafolecimab, marketed in China under the brand name SINTBILO®, represents a significant therapeutic advancement in the management of hypercholesterolemia and mixed dyslipidemia.[1] It is a novel, fully human immunoglobulin G2 (IgG2) monoclonal antibody engineered to target and inhibit Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9), a key regulator of cholesterol homeostasis.[3] Developed by Innovent Biologics, Tafolecimab is the first domestically developed PCSK9 inhibitor to receive regulatory approval in China, marking a milestone for the region's biopharmaceutical industry.[6]

The core mechanism of Tafolecimab involves high-affinity binding to circulating PCSK9, thereby preventing the PCSK9-mediated degradation of the Low-Density Lipoprotein Receptor (LDLR) on hepatocyte surfaces.[8] This action enhances LDLR recycling and increases the liver's capacity to clear atherogenic lipoproteins from the bloodstream. Clinically, this translates into robust, significant, and durable reductions in Low-Density Lipoprotein Cholesterol (LDL-C) levels, with pivotal trials demonstrating mean reductions exceeding 60% compared to placebo.[3] Furthermore, Tafolecimab confers beneficial effects on the broader lipid profile, significantly lowering other established cardiovascular risk factors such as Apolipoprotein B (ApoB), non-High-Density Lipoprotein Cholesterol (non-HDL-C), and, notably, Lipoprotein(a) [Lp(a)].[4]