title: Development and validation of a UPLC-MS/MS method for simultaneous determination of fotagliptin and its two major metabolites in human plasma and urine.
abstract: OBJECTIVE
  Fotagliptin is a novel dipeptidyl peptidase IV inhibitor under clinical development for the treatment of Type II diabetes mellitus. The objective of this study was to develop and validate a specific and sensitive ultra-performance liquid chromatography (UPLC)-MS/MS method for simultaneous determination of fotagliptin and its two major metabolites in human plasma and urine. Methodology & results: After being pretreated using an automatized procedure, the plasma and urine samples were separated and detected using a UPLC-ESI-MS/MS method, which was validated following the international guidelines.
  
  
  CONCLUSIONS
  A selective and sensitive UPLC-MS/MS method was first developed and validated for quantifying fotagliptin and its metabolite in human plasma and urine. The method was successfully applied to support the clinical study of fotagliptin in Chinese healthy subjects.
authors.affiliation: Phase I Unit, Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100032, China.
authors.forename: Zhenlei
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Phase I Unit, Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100032, China.
authors.forename: Ji
authors.initials: J
authors.lastname: Jiang
authors.affiliation: Phase I Unit, Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100032, China.
authors.forename: Pei
authors.initials: P
authors.lastname: Hu
authors.affiliation: Phase I Unit, Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100032, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhao
mesh_terms: D001331:Automation; D002138:Calibration; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy / Q000652:urine; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry*; D006801:Humans; D016014:Linear Models; D010880:Piperidines / Q000097:blood* / Q000652:urine*; D011480:Protease Inhibitors / Q000097:blood* / Q000652:urine*; D011786:Quality Control; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D053719:Tandem Mass Spectrometry / Q000379:methods*; D014227:Triazines / Q000097:blood* / Q000652:urine*
chemical_list: D010880:Piperidines; D011480:Protease Inhibitors; D014227:Triazines; C000614744:fotagliptin; D018819:Dipeptidyl Peptidase 4
keywords: DPP-4 inhibitor; UPLC–MS/MS; fotagliptin; human plasma; human urine