1.
J Labelled Comp Radiopharm
; 56(12): 600-8, 2013 Oct.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24285236
RESUMO
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.