Potent small molecule inhibitors of one biosynthetic enzyme, Oxidosqualene Cyclase (OSC), have been identified, and RO 48–8071 (4′-[6-(allylmethylamino)hexyloxy]-4-bromo-2′-fluorobenzophenone fumarate) (RO), has emerged as a useful chemotherapeutic agent for breast and prostate cancer. The gene discussed is LSS; the disease is prostate carcinoma.