Drug intelligence / Profile preview

E28362

Development stage
Preclinical
Lead developer
Shanghai Institute of Materia Medica
Modality
Small Molecules
Administration
Oral
01

Overview

E28362 is a novel small-molecule inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It selectively binds to PCSK9, blocks its interaction with the low-density lipoprotein receptor (LDLR), and promotes PCSK9 degradation through the ubiquitin-proteasome pathway. This increases LDLR levels on hepatic cells, significantly decreases plasma LDL-C (low-density lipoprotein cholesterol), total cholesterol, triglycerides, and PCSK9 levels, and reduces atherosclerotic lesion formation in animal models. E28362 has demonstrated efficacy in ameliorating hyperlipidemia and atherosclerosis in preclinical studies and is considered a promising lead compound for the treatment of hypercholesterolemia and atherosclerosis[1][3][4][7][8].

02

Targets

PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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