Everett J Perkins

Summary

Affiliation: Eli Lilly and Company
Country: USA

Publications

  1. ncbi request reprint Pharmacokinetics, metabolism, and excretion of the intestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S,2S,5R,6S)-2-[(2'S)-(2-amino)propionyl]aminobicyclo[3.1.0.]hexen-2,6-dicarboxylic acid (LY544344) in rats and dogs: assessment of first-pass
    Everett J Perkins
    Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 35:1903-9. 2007
  2. doi request reprint Characterization of the expression and activity of carboxylesterases 1 and 2 from the beagle dog, cynomolgus monkey, and human
    Eric T Williams
    Department of Drug Disposition, Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 39:2305-13. 2011
  3. doi request reprint The biotransformation of prasugrel, a new thienopyridine prodrug, by the human carboxylesterases 1 and 2
    Eric T Williams
    Department of Drug Disposition, Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 36:1227-32. 2008
  4. doi request reprint Genomic analysis of the carboxylesterases: identification and classification of novel forms
    Eric T Williams
    Department of Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Phylogenet Evol 57:23-34. 2010
  5. doi request reprint Efficacy of low-dose oral metronomic dosing of the prodrug of gemcitabine, LY2334737, in human tumor xenografts
    Susan E Pratt
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Cancer Ther 12:481-90. 2013
  6. doi request reprint Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption
    Shobha N Bhattachar
    Pharmaceutical Sciences R and D, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Pharm Sci 100:4756-65. 2011
  7. ncbi request reprint Improved bioavailability of the mGlu2/3 receptor agonist LY354740 using a prodrug strategy: in vivo pharmacology of LY544344
    Linda M Rorick-Kehn
    Neuroscience Discovery Research Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Pharmacol Exp Ther 316:905-13. 2006
  8. doi request reprint Synthesis, crystallization, and biological evaluation of an orally active prodrug of gemcitabine
    David M Bender
    Lilly Research Laboratories, Eli Lilly and Co, Indianapolis, Indiana 46285, USA
    J Med Chem 52:6958-61. 2009
  9. pmc Using dried blood spot sampling to improve data quality and reduce animal use in mouse pharmacokinetic studies
    Enaksha R Wickremsinhe
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    J Am Assoc Lab Anim Sci 54:139-44. 2015
  10. doi request reprint Dried blood spot sampling: coupling bioanalytical feasibility, blood-plasma partitioning and transferability to in vivo preclinical studies
    Enaksha R Wickremsinhe
    Lilly Research Laboratories, Eli Lilly and Company, IN, USA
    Bioanalysis 3:1635-46. 2011

Collaborators

Detail Information

Publications11

  1. ncbi request reprint Pharmacokinetics, metabolism, and excretion of the intestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S,2S,5R,6S)-2-[(2'S)-(2-amino)propionyl]aminobicyclo[3.1.0.]hexen-2,6-dicarboxylic acid (LY544344) in rats and dogs: assessment of first-pass
    Everett J Perkins
    Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 35:1903-9. 2007
    ..These results demonstrate the nearly ideal prodrug properties of LY544344 and further validate the utility of the peptide transporter-directed approach to prodrug design...
  2. doi request reprint Characterization of the expression and activity of carboxylesterases 1 and 2 from the beagle dog, cynomolgus monkey, and human
    Eric T Williams
    Department of Drug Disposition, Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 39:2305-13. 2011
    ..Loperamide, a selective human CES2 inhibitor, was also found to be a CES2-selective inhibitor in both dog and monkey. This is the first study to examine substrate specificity among dog, human, and monkey CESs...
  3. doi request reprint The biotransformation of prasugrel, a new thienopyridine prodrug, by the human carboxylesterases 1 and 2
    Eric T Williams
    Department of Drug Disposition, Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 36:1227-32. 2008
    ..These data help explain the rapid appearance of R-138727 in human plasma, where maximum concentrations are observed 0.5 h after a prasugrel p.o. dose, and the rapid onset of action of prasugrel...
  4. doi request reprint Genomic analysis of the carboxylesterases: identification and classification of novel forms
    Eric T Williams
    Department of Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Phylogenet Evol 57:23-34. 2010
    ..Finally, this study presents considerations for a broader phylogenetic-based nomenclature that could encompass other serine hydrolases in addition to the CEs...
  5. doi request reprint Efficacy of low-dose oral metronomic dosing of the prodrug of gemcitabine, LY2334737, in human tumor xenografts
    Susan E Pratt
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Cancer Ther 12:481-90. 2013
    ..Thus, metronomic oral low-dose LY2334737 is efficacious, well tolerated, and easily combined with capecitabine for improved efficacy. Elevated CES2 or ENT1 expression may enhance LY2334737 tumor response...
  6. doi request reprint Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption
    Shobha N Bhattachar
    Pharmaceutical Sciences R and D, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Pharm Sci 100:4756-65. 2011
    ..Pharmacokinetic experiments were conducted in dogs to evaluate the effect of gastric pH modification on plasma exposure. The data were qualitatively consistent with the predictions...
  7. ncbi request reprint Improved bioavailability of the mGlu2/3 receptor agonist LY354740 using a prodrug strategy: in vivo pharmacology of LY544344
    Linda M Rorick-Kehn
    Neuroscience Discovery Research Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Pharmacol Exp Ther 316:905-13. 2006
    ..The present data confirm that mGlu2/3 receptor agonists produce antipsychotic and anxiolytic effects in animal behavioral models and demonstrate that oral bioavailability of LY354740 was substantially increased using a prodrug strategy...
  8. doi request reprint Synthesis, crystallization, and biological evaluation of an orally active prodrug of gemcitabine
    David M Bender
    Lilly Research Laboratories, Eli Lilly and Co, Indianapolis, Indiana 46285, USA
    J Med Chem 52:6958-61. 2009
    ..The compound has entered clinical trials and is being evaluated as a potential new anticancer agent...
  9. pmc Using dried blood spot sampling to improve data quality and reduce animal use in mouse pharmacokinetic studies
    Enaksha R Wickremsinhe
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    J Am Assoc Lab Anim Sci 54:139-44. 2015
    ....
  10. doi request reprint Dried blood spot sampling: coupling bioanalytical feasibility, blood-plasma partitioning and transferability to in vivo preclinical studies
    Enaksha R Wickremsinhe
    Lilly Research Laboratories, Eli Lilly and Company, IN, USA
    Bioanalysis 3:1635-46. 2011
    ..The adoption of dried blood spot (DBS) sampling and analysis to support drug discovery and development requires the understanding of its bioanalytical feasibility as well as the distribution of the analyte in blood...
  11. doi request reprint Effect of buffer components and carrier solvents on in vitro activity of recombinant human carboxylesterases
    Eric T Williams
    Department of Drug Disposition, Lilly Research, Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States
    J Pharmacol Toxicol Methods 57:138-44. 2008
    ..Therefore, it is unknown if the many different assay conditions used by various laboratories have a substantial impact on the activity of CE enzymes...