Squalene synthase inhibitors 1998

Abstract

Squalene synthase, the first enzyme in the cholesterol biosynthetic pathway dedicated to sterol synthesis, represents an attractive target for hypocholesterolaemic therapy. Whilst no squalene synthase inhibitors have yet reached clinical trials, the most advanced compounds in this class, exemplified by J-104,123 and RPR 107393, reduce plasma cholesterol following chronic oral dosing in animal models. This review summarises the recent patent and primary literature in this field.

• cholesterol biosynthesis
• hypocholesterolaemia
• squalene synthase