Identification and characterisation of cytochrome-p450 metabolites of the ozonide antimalarial drug candidate oz439 (using chemical derivatisation and lc/ms)

• In: Posters C - Drug Design and Discovery
• At: PSWC, Melbourne (Australia) (2014)
• Type: Poster
• Poster code: PC-003
• By: CHIU, Francis (Monash University, CDCO, MIPS, Parkville, Australia)
• Co-author(s): Wang, Xiaofang (College of Pharmacy, University of Nebraska Medical Center, Nebraska, United States of America)
  Zhou, Lin (College of Pharmacy, University of Nebraska Medical Center, Nebraska, United States of America)
  Sriraghavan, Kamaraj (College of Pharmacy, University of Nebraska Medical Center, Nebraska, United States of America)
  Alker, Andr (F. Hoffmann-La Roche Ltd, Basel, Switzerland)
  Ruf, Armin (F. Hoffmann-La Roche Ltd, Basel, Switzerland)
  Matile, Hugues (F. Hoffmann-La Roche Ltd, Basel, Switzerland)
  Dong, Yuxiang (College of Pharmacy, University of Nebraska Medical Center, Nebraska, United States of America)
  Wittlin, Sergio (Swiss Tropical and Public Health Institute, Basel, Switzerland)
  Scheurer, Christian (Swiss Tropical and Public Health Institute, Basel, Switzerland)
  Vennerstrom, Jonathan (College of Pharmacy, University of Nebraska Medical Center, Nebraska, United States of America)
  Charman, Susan (Monash University, Parkville, Australia)
  
• Abstract:

  Background: OZ439 is a second generation synthetic ozonide that has the potential to provide a single oral dose cure of malaria. Aim: To identify and characterise OZ439 metabolites generated in human liver microsomes (HLM) to guide the synthesis of metabolite standards for the characterisation of the human metabolite profile. Methods: OZ439 was..

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