Obicetrapib
CETP pathophysiology and inhibition, an update: the drug class biology, trial status and adverse effects surveyed before obicetrapib phase 3 (Drug Discov Today 2021)
Original title: Pathophysiology and inhibition of cholesteryl ester transfer protein for prevention of cardiovascular diseases: An update
A review of cholesteryl ester transfer protein (CETP) pathophysiology and the drug class designed to inhibit it, including anacetrapib, torcetrapib and obicetrapib among others. The authors describe how CETP inhibition raises HDL particles and lowers LDL, altering cholesterol transport in ways intended to reduce atherosclerosis, and survey the trial status, adverse effects and limitations of the various inhibitors developed. A general pathophysiology and status overview written before the phase 3 readouts for obicetrapib, without a specific obicetrapib efficacy figure of its own.
Original abstract
The enzyme cholesteryl ester transfer protein (CETP), involved in cholesterol metabolism and transportation, is one of the main causes of cardiovascular (CV) disease (CVD). When the CETP concentration is decreased by CETP inhibitors (e.g., anacetrapib, torcetrapib, obicetrapib, etc.), high-density lipoprotein (HDL) particles are formed and low-density lipoprotein (LDL) is decreased along with cholesterol transportation alteration, which reduces the development of atherosclerosis. Here, we discuss the role of CETP inhibitors in reducing well-known 'bad' cholesterols and the current status of trials of different CETP inhibitors, their adverse effects, and limitations, as well as the pathophysiology of CETP.
the classmechanismsobicetrapib
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.