Squalene synthase, the first enzyme in the cholesterol biosynthetic pa
thway dedicated to sterol synthesis, represents an attractive target f
or hypocholesterolaemic therapy. Whilst no squalene synthase inhibitor
s have yet reached clinical trials, the most advanced compounds in thi
s class, exemplified by J-104,123 and RPR 107393, reduce plasma choles
terol following chronic oral dosing in animal models. This review summ
arises the recent patent and primary literature in this field.