Pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor PHX1149: double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects.

@article{OFarrell2007PharmacokineticAP,
  title={Pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor PHX1149: double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects.},
  author={A Marie O'Farrell and Andre A van Vliet and Khalid Abou Farha and Julie M. Cherrington and David Campbell and Xinqiang Li and Denise Hanway and Jianke Li and H P Guler},
  journal={Clinical therapeutics},
  year={2007},
  volume={29 8},
  pages={
          1692-705
        }
}
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An overview of published patents describing natural and synthetic DPP-4 inhibitors from January 2015 to December 2018 is provided to address the pancreas-related adverse events as well as their impact on cardiovascular outcomes via long-term studies.
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In patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses was associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitgliptin concentration of 100 nm or greater and an augmentation of active GLP-1 and GIP levels of 2-fold or higher after an OGTT.
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus
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Sitagliptin significantly improved glycaemia control and was well tolerated in patients with type 2 diabetes mellitus who had inadequate glycaemic control on exercise and diet.
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In nondiabetic obese subjects, treatment with sitagliptin 200 mg bid was generally well tolerated without associated hypoglycemia and led to maximal inhibition of plasma DPP‐4 activity, increased active GLP‐1, and reduced glycemic excursion.
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