Sabrina X Zhao

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi request reprint Simple strategies for reducing sample loads in in vitro metabolic stability high-throughput screening experiments: a comparison between traditional, two-time-point and pooled sample analyses
    Sabrina X Zhao
    Candidate Enhancement Group, Exploratory Medicinal Sciences, Pfizer Inc, Eastern Point Road MS 8118W 102, Groton, Connecticut 06340, USA
    J Pharm Sci 94:38-45. 2005
  2. ncbi request reprint Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4
    Amit S Kalgutkar
    Pharmacokinetics Dynamics and Metabolism Department, Pfizer Global Research and Development, Eastern Point Road, Groton, MA 06340, USA
    Chem Biol Interact 155:10-20. 2005
  3. doi request reprint Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose
    R Scott Obach
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 21:1814-22. 2008
  4. ncbi 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. doi request reprint Can in vitro metabolism-dependent covalent binding data distinguish hepatotoxic from nonhepatotoxic drugs? An analysis using human hepatocytes and liver S-9 fraction
    Jonathon N Bauman
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 22:332-40. 2009
  6. ncbi request reprint A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 20:1954-65. 2007
  7. doi request reprint Metabolism of a dopamine receptor partial agonist in rats, including an unusual N-dearylation reaction
    Sabrina X Zhao
    Pfizer Inc, Groton, U S
    Drug Metab Pharmacokinet 26:266-79. 2011
  8. ncbi request reprint NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine
    Sabrina X Zhao
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut, USA
    Chem Res Toxicol 20:1649-57. 2007
  9. ncbi request reprint Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human
    Amit S Kalgutkar
    Pharmacokinetics, Dyamics, and Metabolism Department, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Drug Metab Dispos 35:2111-8. 2007
  10. 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

Collaborators

Detail Information

Publications13

  1. ncbi request reprint Simple strategies for reducing sample loads in in vitro metabolic stability high-throughput screening experiments: a comparison between traditional, two-time-point and pooled sample analyses
    Sabrina X Zhao
    Candidate Enhancement Group, Exploratory Medicinal Sciences, Pfizer Inc, Eastern Point Road MS 8118W 102, Groton, Connecticut 06340, USA
    J Pharm Sci 94:38-45. 2005
    ..98 and 0.97, respectively. Both methods have the potential to: 1. produce data of similar quality to traditional high throughput ADME assays, 2. be easily implemented, 3. shorten analytical run times, and 4. be reproducible and robust...
  2. ncbi request reprint Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4
    Amit S Kalgutkar
    Pharmacokinetics Dynamics and Metabolism Department, Pfizer Global Research and Development, Eastern Point Road, Groton, MA 06340, USA
    Chem Biol Interact 155:10-20. 2005
    ..It is proposed that the quinone-imine and/or the epoxide intermediate(s) may represent a rate-limiting step in the initiation of trazodone-mediated hepatotoxicity...
  3. doi request reprint Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose
    R Scott Obach
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 21:1814-22. 2008
    ....
  4. ncbi 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. doi request reprint Can in vitro metabolism-dependent covalent binding data distinguish hepatotoxic from nonhepatotoxic drugs? An analysis using human hepatocytes and liver S-9 fraction
    Jonathon N Bauman
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 22:332-40. 2009
    ..will be essential to any understanding of the problem of metabolism-dependent hepatotoxicity and predicting toxicity from in vitro experiments...
  6. ncbi request reprint A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Chem Res Toxicol 20:1954-65. 2007
    ..These structural changes not only abrogated the bioactivation liability associated with 1 but also resulted in compounds that retained the attractive pharmacological and pharmacokinetic attributes of the prototype agent...
  7. doi request reprint Metabolism of a dopamine receptor partial agonist in rats, including an unusual N-dearylation reaction
    Sabrina X Zhao
    Pfizer Inc, Groton, U S
    Drug Metab Pharmacokinet 26:266-79. 2011
    ..An additional mechanism involves oxidation of the naphthol metabolite via a radical mechanism, since this metabolite was also shown to undergo N-dearylation...
  8. ncbi request reprint NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine
    Sabrina X Zhao
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, Connecticut, USA
    Chem Res Toxicol 20:1649-57. 2007
    ....
  9. ncbi request reprint Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human
    Amit S Kalgutkar
    Pharmacokinetics, Dyamics, and Metabolism Department, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Drug Metab Dispos 35:2111-8. 2007
    ....
  10. 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
    ....
  11. ncbi request reprint Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationsh
    Donn G Wishka
    Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 49:4425-36. 2006
    ....
  12. ncbi request reprint High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models
    Cornelis E C A Hop
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Curr Drug Metab 9:847-53. 2008
    ..Finally, in vitro ADME screening can generate large quantities of data obtained under identical conditions to allow building of reliable in silico models...
  13. ncbi request reprint Bioactivation of the nontricyclic antidepressant nefazodone to a reactive quinone-imine species in human liver microsomes and recombinant cytochrome P450 3A4
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 33:243-53. 2005
    ....