ATR-101 (PD 132301-02; Nevanimibe HCl) is an orally active, potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT1, SOAT1) inhibtior (IC50 = 52 nM; intestinal microsome from cholesterol-fed rabbits) th at reduces plasma cholesterol in both acute (by 77%; 50 mg/kg po.) and chronic (by 80%; 10 mg/kg po.) cholesterol-fed r at models. In addition, ATR-101 is reported to exhibit therapeutic efficacy against adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH), and Cushingμs syndrome (CS).
