Review collates the bioanalytical methods developed to quantify anacetrapib, dalcetrapib, and torcetrapib in biological samples (Biomed Chromatogr 2013)

Clinical investigations of choleteryl ester transfer protein (CETP) inhibitors are still underway owing to its promise of reducing risk factors in patients with cardiovascular disease. Although several CETP inhibitors have reached late phase clinical testing, there is a paucity of publications that describe the determination of various CETP inhibitors in human and/or animal matrices. An attempt is made in this review to collate bioanalytical information on three CETP inhibitors (anacetrapib, dalcetrapib and torcetrapib) and its metabolites, where data were available and reported. As elaborated in the review, owing to numerous structural issues coupled with chromatography/detection challenges indigenous to the class, a wide array of analytical tools, detection systems, interesting process manipulations and separation nuances have been utilized for the quantitative analysis of CETP inhibitors and applicable metabolites.