Jonathan N Bauman

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi request reprint Udp-glucuronosyltransferase 2b7 is the major enzyme responsible for gemcabene glucuronidation in human liver microsomes
    Jonathan N Bauman
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Drug Metab Dispos 33:1349-54. 2005
  2. ncbi request reprint Atorvastatin glucuronidation is minimally and nonselectively inhibited by the fibrates gemfibrozil, fenofibrate, and fenofibric acid
    Theunis C Goosen
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA
    Drug Metab Dispos 35:1315-24. 2007
  3. doi request reprint Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors
    Robert L Walsky
    Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc, Groton, Connecticut 06340, USA
    Drug Metab Dispos 40:1051-65. 2012
  4. doi request reprint Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatme
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics and Metabolism Department and Department of Medicinal Chemistry, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 23:1115-26. 2010
  5. pmc Limited influence of UGT1A1*28 and no effect of UGT2B7*2 polymorphisms on UGT1A1 or UGT2B7 activities and protein expression in human liver microsomes
    Vincent C Peterkin
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Br J Clin Pharmacol 64:458-68. 2007
  6. doi request reprint Utility of MetaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-N-phenethyl-acetamide
    David Boyer
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 37:999-1008. 2009
  7. doi request reprint Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation
    Daniel P Walker
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 18:6071-7. 2008
  8. ncbi request reprint The effect of bergamottin on diazepam plasma levels and P450 enzymes in beagle dogs
    Jasminder Sahi
    Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Drug Metab Dispos 30:135-40. 2002
  9. ncbi request reprint Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity
    Abdul E Mutlib
    Department of Pharmacokinetics, Pfizer Inc, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA
    Chem Res Toxicol 19:701-9. 2006
  10. doi request reprint Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists
    Amit S Kalgutkar
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 19:1559-63. 2009

Detail Information

Publications11

  1. ncbi request reprint Udp-glucuronosyltransferase 2b7 is the major enzyme responsible for gemcabene glucuronidation in human liver microsomes
    Jonathan N Bauman
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Drug Metab Dispos 33:1349-54. 2005
    ..In conclusion, using the three independent experimental approaches typically used for cytochrome P450 reaction phenotyping, UGT2B7 is the major enzyme contributing to gemcabene glucuronidation in human liver microsomes...
  2. ncbi request reprint Atorvastatin glucuronidation is minimally and nonselectively inhibited by the fibrates gemfibrozil, fenofibrate, and fenofibric acid
    Theunis C Goosen
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA
    Drug Metab Dispos 35:1315-24. 2007
    ..2-fold) after gemfibrozil coadministration and no interaction with fenofibrate. This result is consistent with recent clinical reports indicating minimal atorvastatin AUC increases ( approximately 1.2- to 1.4-fold) with gemfibrozil...
  3. doi request reprint Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors
    Robert L Walsky
    Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer Inc, Groton, Connecticut 06340, USA
    Drug Metab Dispos 40:1051-65. 2012
    ....
  4. doi request reprint Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatme
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics and Metabolism Department and Department of Medicinal Chemistry, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 23:1115-26. 2010
    ..Herein, the collective findings from our discovery efforts in the CaSR program, which include the incorporation of appropriate derisking steps when dealing with RM issues are summarized...
  5. pmc Limited influence of UGT1A1*28 and no effect of UGT2B7*2 polymorphisms on UGT1A1 or UGT2B7 activities and protein expression in human liver microsomes
    Vincent C Peterkin
    Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Br J Clin Pharmacol 64:458-68. 2007
    ....
  6. doi request reprint Utility of MetaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-N-phenethyl-acetamide
    David Boyer
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 37:999-1008. 2009
    ..Overall, the predictions from MetaSite gave useful information leading to the design of new compounds with improved metabolic properties...
  7. doi request reprint Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation
    Daniel P Walker
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 18:6071-7. 2008
    ....
  8. ncbi request reprint The effect of bergamottin on diazepam plasma levels and P450 enzymes in beagle dogs
    Jasminder Sahi
    Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Drug Metab Dispos 30:135-40. 2002
    ..In jejunal microsomes, CYP3A12 activity doubled with bergamottin treatment. CYP2B11, CYP1A1/2 activity and tolbutamide hydroxylation was not detected. In conclusion, bergamottin is both an inhibitor and an inducer of P450 enzymes...
  9. ncbi request reprint Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity
    Abdul E Mutlib
    Department of Pharmacokinetics, Pfizer Inc, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA
    Chem Res Toxicol 19:701-9. 2006
    ..This synergistic increase in toxicity is postulated to be due to inhibition of UGTs (1A6, 1A9, and 2B15) responsible for detoxifying APAP through the glucuronidation pathway...
  10. doi request reprint Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists
    Amit S Kalgutkar
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 19:1559-63. 2009
    ..Plausible hypotheses that can collectively account for the differences in mutagenic response of the two piperazine analogs are discussed...
  11. doi request reprint Comparison of the bioactivation potential of the antidepressant and hepatotoxin nefazodone with aripiprazole, a structural analog and marketed drug
    Jonathan N Bauman
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 36:1016-29. 2008
    ..This attribute probably reduces the total body burden to reactive metabolite exposure and may not exceed a threshold needed for toxicity...