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Amit S. Kalgutkar

Pharmacokinetics

Dynamics

and Metabolism Department

Pfizer Worldwide Research and Development

[email]@pfizer.com

Name/email consistency: high

 
 
 
 
 
 
 

Affiliation

  • Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Worldwide Research and Development. 2005 - 2012

References

  1. Drug discovery for a new generation of covalent drugs. Kalgutkar, A.S., Dalvie, D.K. Expert. Opin. Drug. Discov (2012) [Pubmed]
  2. Immune-Mediated Agranulocytosis Caused by the Cocaine Adulterant Levamisole: A Case for Reactive Metabolite(s) Involvement. Wolford, A., McDonald, T.S., Eng, H., Hansel, S., Chen, Y., Bauman, J., Sharma, R., Kalgutkar, A.S. Drug Metab. Dispos. (2012) [Pubmed]
  3. Preclinical Species and Human Disposition of PF-04971729, a Selective Inhibitor of the Sodium-Dependent Glucose Cotransporter 2 and Clinical Candidate for the Treatment of Type 2 Diabetes Mellitus. Kalgutkar, A.S., Tugnait, M., Zhu, T., Kimoto, E., Miao, Z., Mascitti, V., Yang, X., Tan, B., Walsky, R.L., Chupka, J., Feng, B., Robinson, R.P. Drug Metab. Dispos. (2011) [Pubmed]
  4. Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro. Kalgutkar, A.S., Mascitti, V., Sharma, R., Walker, G.W., Ryder, T., McDonald, T.S., Chen, Y., Preville, C., Basak, A., McClure, K.F., Kohrt, J.T., Robinson, R.P., Munchhof, M.J., Cornelius, P. Chem. Res. Toxicol. (2011) [Pubmed]
  5. 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 treatment of osteoporosis. Kalgutkar, A.S., Griffith, D.A., Ryder, T., Sun, H., Miao, Z., Bauman, J.N., Didiuk, M.T., Frederick, K.S., Zhao, S.X., Prakash, C., Soglia, J.R., Bagley, S.W., Bechle, B.M., Kelley, R.M., Dirico, K., Zawistoski, M., Li, J., Oliver, R., Guzman-Perez, A., Liu, K.K., Walker, D.P., Benbow, J.W., Morris, J. Chem. Res. Toxicol. (2010) [Pubmed]
  6. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. Kalgutkar, A.S., Frederick, K.S., Chupka, J., Feng, B., Kempshall, S., Mireles, R.J., Fenner, K.S., Troutman, M.D. J. Pharm. Sci (2009) [Pubmed]
  7. Structural alerts, reactive metabolites, and protein covalent binding: how reliable are these attributes as predictors of drug toxicity?. Kalgutkar, A.S., Didiuk, M.T. Chem. Biodivers. (2009) [Pubmed]
  8. 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. Kalgutkar, A.S., Feng, B., Nguyen, H.T., Frederick, K.S., Campbell, S.D., Hatch, H.L., Bi, Y.A., Kazolias, D.C., Davidson, R.E., Mireles, R.J., Duignan, D.B., Choo, E.F., Zhao, S.X. Drug Metab. Dispos. (2007) [Pubmed]
  9. A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif. Kalgutkar, A.S., Driscoll, J., Zhao, S.X., Walker, G.S., Shepard, R.M., Soglia, J.R., Atherton, J., Yu, L., Mutlib, A.E., Munchhof, M.J., Reiter, L.A., Jones, C.S., Doty, J.L., Trevena, K.A., Shaffer, C.L., Ripp, S.L. Chem. Res. Toxicol. (2007) [Pubmed]
  10. Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation. Kalgutkar, A.S., Dalvie, D.K., Aubrecht, J., Smith, E.B., Coffing, S.L., Cheung, J.R., Vage, C., Lame, M.E., Chiang, P., McClure, K.F., Maurer, T.S., Coelho, R.V., Soliman, V.F., Schildknegt, K. Drug Metab. Dispos. (2007) [Pubmed]
  11. Mechanism-based inactivation of cytochrome P450 enzymes: chemical mechanisms, structure-activity relationships and relationship to clinical drug-drug interactions and idiosyncratic adverse drug reactions. Kalgutkar, A.S., Obach, R.S., Maurer, T.S. Curr. Drug Metab. (2007) [Pubmed]
  12. Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes. Kalgutkar, A.S., Hatch, H.L., Kosea, F., Nguyen, H.T., Choo, E.F., McClure, K.F., Taylor, T.J., Henne, K.R., Kuperman, A.V., Dombroski, M.A., Letavic, M.A. Biopharm. Drug. Dispos (2006) [Pubmed]
  13. Minimising the potential for metabolic activation in drug discovery. Kalgutkar, A.S., Soglia, J.R. Expert. Opin. Drug. Metab. Toxicol (2005) [Pubmed]
 
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