Prediction of CYP Down Regulation after Tusamitamab Ravtansine Administration (a DM4‐Conjugate), Based on an In Vitro–In Vivo Extrapolation Approach
Clemence Pouzin,
Donato Teutonico,
Nathalie Fagniez
et al.
Abstract:Tusamitamab ravtansine is an antibody‐drug conjugate (ADC) composed of a humanized monoclonal antibody (IgG1) and DM4 payload. Even if DM4 and its main metabolite Methyl‐DM4 (Me‐DM4) circulate at low concentrations after ADC administration, their potential as perpetrators of cytochrome P450 mediated drug‐drug interaction (DDI) was assessed. In vitro studies in human hepatocytes indicated that Me‐DM4 elicited a clear concentration‐dependent down regulation of cytochrome P450 enzymes (CYP3A4, 1A2, 2B6). Since DM… Show more
Set email alert for when this publication receives citations?
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.