DMD #47316 Metabolism, Excretion, and Pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4- (pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a DPP-IV Inhibitor, in Rat, Dog and Human

نویسندگان

  • Raman Sharma
  • Hao Sun
  • David W. Piotrowski
  • Tim F. Ryder
  • Shawn D. Doran
  • Haiqing Dai
  • Chandra Prakash
چکیده

246 Introduction: 469 Discussion: 1447 References: 24 Tables: 6 Figures: 11 Abbreviations: DPP-IV, dipeptidyl peptidase IV; GLP-1 glucogen-like peptide 1; PF-00734200, 3,3-Difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2yl)methanone, ESI, electrospray ionization; HFAA, hexaflouroacetylacetone; SD, Sprague Dawley; GLP-1, glucagon like peptide; FAP, fibroblast activation protein; APP, aminopeptidase P; POP, propyl oligopeptidase. 2 This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on August 15, 2012 as DOI: 10.1124/dmd.112.047316 at A PE T Jornals on Jne 0, 2017 dm d.aspurnals.org D ow nladed from

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Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human.

The disposition of 3,3-difluoropyrrolidin-1-yl{(2S,4S)-4-[4-(pyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl}methanone (PF-00734200), a dipeptidyl peptidase IV inhibitor that progressed to phase 3 for the treatment of type 2 diabetes, was examined in rats, dogs, and humans after oral administration of a single dose of [(14)C]PF-00734200. Mean recoveries of administered radioactivity were 97.1, 92...

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تاریخ انتشار 2012