Journal of Drug Metabolism & Toxicology
Open Access

Marc Ausburger

Publications

• Research Article
  Detection and Identification of Reactive Drug Metabolites Leading to Idiosyncratic Toxicity: Lapatinib as a Case Example
  Author(s): Rayane Mohamed, Flavia Storelli, Jonathan Sidibe, Nasim Bararpour, Jules Desmeules, Marc Ausburger, Youssef Daali and A Thomas Rayane Mohamed, Flavia Storelli, Jonathan Sidibe, Nasim Bararpour, Jules Desmeules, Marc Ausburger, Youssef Daali and A Thomas
  
  New pharmaceutical drug development requires more than a billion dollars and can take 12 years of research effort. New chemical entities or NCEs can be dropped from development for many reasons during this process, two major reasons being efficacy and toxicity. Lapatinib was approved in 2007 by FDA as an orally active drug against breast cancer. While some advantages were observed over chemotherapy, clinical evidences of idiosyncratic hepatoxicity were reported for this compound. Numerous studies showed that lapatinib was extensively metabolized and the formation of reactive metabolites could be the origin of the observed toxicity. It has been shown that CYP3A are the main drug metabolizing enzymes involved in the metabolism pathway of lapatinib. This study aims to identify and detect potential reactive metabolites of lapatinib formed after in vitro microsomal incubation using a compr.. View More»
  DOI: 10.4172/2157-7609.1000242

  Abstract PDF

Relevant Topics