Characterization of the metabolism of fenretinide by human liver microsomes cytochrome P450 enzymes and UDP-glucuronosyltransferases

摘要

BACKGROUND AND PURPOSEFenretinide (4-HPR) is a retinoic acid analogue, currently used in clinical trials in oncology. Metabolism of 4-HPR is of particular interest due to production of the active metabolite 4′-oxo 4-HPR and the clinical challenge of obtaining consistent 4-HPR plasma concentrations in patients. Here, we assessed the enzymes involved in various 4-HPR metabolic pathways.