Anacetrapib
Viewpoint charts efforts to optimize anacetrapib into a best-in-class CETP inhibitor (J Med Chem 2021)
Original title: Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP)
CETP inhibitors raise HDL levels in human clinical trials, but the first generation of these drugs either proved toxic in pivotal trials or delivered minimal therapeutic benefit. Anacetrapib showed some clinical benefit but is highly lipophilic, a property with pharmacokinetic drawbacks including tissue accumulation. This viewpoint highlights medicinal chemistry efforts aimed at optimizing the anacetrapib chemical scaffold to produce a best-in-class CETP inhibitor that retains its clinical efficacy while improving on its physicochemical liabilities.
Original abstract
Inhibitors of cholesteryl ester transfer protein (CETP) elevate HDL levels human clinical trials. However, the first CETP inhibitors proved toxic in pivotal trials or showed minimal therapeutic benefit. Anacetrapib showed some clinical benefit but is high lipophilic. This Viewpoint highlights efforts to optimize anacetrapib to a best-in-class CETP inhibitor.
anacetrapibthe classpharmacology
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.