A phase I trial of GMX1777, an inhibitor of nicotinamide phosphoribosyl transferase (NAMPRT), given as a 24-hour infusion.

  title={A phase I trial of GMX1777, an inhibitor of nicotinamide phosphoribosyl transferase (NAMPRT), given as a 24-hour infusion.},
  author={Michael J. Pishvaian and John L. Marshall and J. J. Hwang and Shakun M. Malik and Aiwu Ruth He and John F Deeken and C. B. Kelso and Ion Cotarla and Mark S. Berger},
  journal={Journal of clinical oncology : official journal of the American Society of Clinical Oncology},
  volume={27 15\_suppl},
  • M. Pishvaian, J. Marshall, +6 authors M. Berger
  • Published 2009
  • Chemistry, Medicine
  • Journal of clinical oncology : official journal of the American Society of Clinical Oncology
3581 Background: GMX1777 is a pro-drug which converts to GMX1778, a potent and specific small molecule inhibitor of NAMPRT, the rate-limiting enzyme in NAD+ synthesis. NAMPRT activity is increased in tumor cells dependent on the glycolytic pathway. The aims of this first-in-man study were to define a dose of GMX1777 administered by 24-hr infusion with acceptable safety for phase II studies, and to determine the pharmacokinetic (PK) parameters of both GMX1777 and GMX1778. METHODS GMX1777 was… Expand
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