Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction

DE Gutstein, R Krishna, D Johns… - Clinical …, 2012 - Wiley Online Library
DE Gutstein, R Krishna, D Johns, HK Surks, HM Dansky, S Shah, YB Mitchel, J Arena…
Clinical Pharmacology & Therapeutics, 2012Wiley Online Library
Cholesteryl ester transfer protein (CETP) inhibition is a promising experimental strategy to
raise high‐density lipoprotein cholesterol (HDL‐C) and reduce cardiovascular risk. This
review focuses on the highly selective and potent CE TP inhibitor anacetrapib and discusses
the available preclinical and clinical information pertaining to it. We also describe strategies
to target HDL‐C, discuss the mechanism underlying CETP inhibition and its effects on lipid
biology, and give an overview of other CETP inhibitors that are currently in development …
Cholesteryl ester transfer protein (CETP) inhibition is a promising experimental strategy to raise high‐density lipoprotein cholesterol (HDL‐C) and reduce cardiovascular risk. This review focuses on the highly selective and potent CE TP inhibitor anacetrapib and discusses the available preclinical and clinical information pertaining to it. We also describe strategies to target HDL‐C, discuss the mechanism underlying CETP inhibition and its effects on lipid biology, and give an overview of other CETP inhibitors that are currently in development.
Clinical Pharmacology & Therapeutics (2012); 91 1, 109–122. doi:10.1038/clpt.2011.271
Wiley Online Library