Anacetrapib
Isotope-labeled anacetrapib and its metabolites are synthesized to support bioavailability and drug-metabolism studies (J Labelled Comp Radiopharm 2013)
Original title: Synthesis of stable isotope labeled anacetrapib, its major metabolites and [(14) C]anacetrapib
Anacetrapib (MK-0859), then in phase III trials for elevated cholesterol and cardiovascular disease prevention, required labeled material to support its clinical development. This paper describes the synthesis of an [M+6]-labeled version of the active pharmaceutical ingredient for use in an absolute bioavailability study, an [M+13]-labeled internal standard, three stable-isotope-labeled metabolites for analyzing clinical samples, and a carbon-14-labeled version of anacetrapib to support drug metabolism studies, providing the labeled reagents needed to characterize the pharmacokinetics and metabolism of anacetrapib in clinical trials.
Original abstract
Cholesteryl ester transfer protein inhibitors are an important class of compounds designed to treat hypocholesterolemia and prevent cardiovascular disease. Anacetrapib (MK-0859) is currently in phase III trials for the treatment of elevated cholesterol levels and prevention of cardiovascular disease. In order to further support the development of anacetrapib, we prepared [M + 6]MK-0859, which was required in support of an absolute bioavailability study of the active pharmaceutical ingredient (API). Additional support included the synthesis of an internal standard [M + 13] and three stable isotope labeled metabolites, which were used to analyze clinical samples, and [(14) C]MK-0859 to support drug metabolism studies.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.