Journal of Drug Metabolism & Toxicology
Open Access

Helen M Grant

Publications

• Research Article
  Identification of Novel Metabolic Pathways of Sitagliptin (STG) by LC/MS and LC/MS2 after Incubations with Rat Hepatocytes
  Author(s): Osama IG Khreit, Helen M Grant, Catherine Henderson, David G Watson and Oliver B Sutcliffec Osama IG Khreit, Helen M Grant, Catherine Henderson, David G Watson and Oliver B Sutcliffec
  
  Sitagliptin (STG), a drug for treating Type Ii Diabetes Mellitus (T2DM), has been associated with severe joint pain in some patients. In this paper the metabolic profile of the drug has been investigated in order to determine metabolism and formation of reactive compounds which may contribute to this adverse effect. Metabolism of STG was investigated in vitro by incubation with freshly isolated Sprague-Dawley rat hepatocytes, to characterize Phase I and II metabolites, and the reaction mixture analysed on a zwitter ionic hydrophilic interaction (ZIC®-HILIC) column using LC-MS and LC-MS2 utilising electrospray ionization (ESI) in the positive ion mode. STG was metabolised to yield eleven metabolites, but in total only 3.1% of the parent drug was metabolised over 2 hrs incubation. These metabolites were structurally characterized on the basis of accurate mass analyses and .. View More»
  DOI: 10.4172/2157-7609.1000220

  Abstract PDF

Relevant Topics