Drug intelligence / Profile preview

probucol

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral
01

Overview

Probucol is a lipid-lowering agent and powerful antioxidant originally developed to prevent the degradation of rubber, later repurposed for medical use to reduce serum low-density lipoprotein cholesterol (LDL-C) levels. It lowers cholesterol by increasing the rate of LDL catabolism and enhancing excretion into bile, independent of the LDL receptor. Probucol also inhibits ABCA1-mediated cellular lipid efflux, which reduces HDL cholesterol (HDL-C) by about 30%, but increases reverse cholesterol transport capacity overall. Its antioxidant properties help prevent oxidation of LDL particles, potentially slowing atherogenesis. The drug was withdrawn from several Western markets due to safety concerns, including QT prolongation[1][2][3][4][5].

Brand names
Lorelco
Other names
probucol
02

Targets

ABCA1 (ATP-binding cassette transporter A1)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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