Correlation Engine 2.0
Clear Search sequence regions

  • blood (1)
  • cetilistat (8)
  • feces (1)
  • free (3)
  • germ free life (1)
  • mass (1)
  • orlistat (1)
  • rats (6)
  • small intestine (1)
  • Sizes of these terms reflect their relevance to your search.

    Cetilistat (CET) is a pancreatic lipase inhibitor approved for management of obesity after the serious adverse effects exhibited by its analogue orlistat. Exhaustive literature review reveals lack of comprehensive reports on its biotransformation. With a view to study the same, the present study reports the identification and characterization of metabolites of CET in rats using UPLC-MS/MS. As the small intestine is the site of action for CET, it is important that the role of microbial flora in the metabolism of CET be explored. To achieve this, the metabolic profile of CET was compared between normal and pseudo-germ-free rats. The study involved the administration of a drug suspension to male Sprague-Dawley pseudo-germ-free and normal untreated rats followed by collection of urine, feces, and blood at specific intervals. Sample preparation was performed using liquid-liquid extraction and concentration of samples followed by analysis using LC-MS/MS. Finally, an in silico study was performed on the drug and metabolites to predict their toxicological properties using ADMET PredictorTM software. Four metabolites of CET were observed in in vivo matrices. As expected, significant changes were observed both qualitatively and quantitatively, implying that formation of metabolites was both CYP enzymes and gut microflora mediated. © 2020 John Wiley & Sons, Ltd.


    Shristy S Tiwari, Sumit Mukesh, Abhay T Sangamwar, M V N Kumar Talluri. In vivo metabolic investigation of cetilistat in normal versus pseudo-germ-free rats using UPLC-QTOFMS/MS and in silico toxicological evaluation of its metabolites. Biomedical chromatography : BMC. 2020 Aug;34(8):e4860

    Expand section icon Mesh Tags

    Expand section icon Substances

    PMID: 32311767

    View Full Text