Anacetrapib was investigated for its potential in cardiovascular disease management but development was discontinued in 2017 by Merck following the REVEAL trial, which showed modest efficacy but raised concerns about long-term safety and off-target effects. It functions as a cholesteryl ester transfer protein (CETP) inhibitor, which helps in increasing high-density lipoprotein (HDL) cholesterol levels while reducing low-density lipoprotein (LDL) cholesterol. This dual action made it a candidate for reducing the risk of heart attacks and strokes in patients with a history of cardiovascular issues. Clinical trials explored its efficacy in combination with statins to enhance cholesterol management. It is not approved for clinical use and is available primarily as a research chemical.