Search Results - "Halladay, Jason S"

A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834 by Sodhi, Jasleen K, Wong, Susan, Kirkpatrick, Donald S, Liu, Lichuan, Khojasteh, S Cyrus, Hop, Cornelis E C A, Barr, John T, Jones, Jeffrey P, Halladay, Jason S

“…GDC-0834, a Bruton's tyrosine kinase inhibitor investigated as a potential treatment of rheumatoid arthritis, was previously reported to be extensively…”
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Comparative assessment of In Vitro-In Vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs by Poulin, Patrick, Hop, Cornelis E C A, Ho, Quynh, Halladay, Jason S, Haddad, Sami, Kenny, Jane R

“…The purpose of this study was to perform a comparative analysis of various in vitro--in vivo extrapolation (IVIVE) methods used for predicting hepatic…”
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Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity by Khojasteh, Siamak Cyrus, Prabhu, Saileta, Kenny, Jane R., Halladay, Jason S., Lu, Anthony Y. H.

“…The majority of marketed small-molecule drugs undergo metabolism by hepatic Cytochrome P450 (CYP) enzymes (Rendic 2002 ). Since these enzymes metabolize a…”
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Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor by LICHUAN LIU, HALLADAY, Jason S, KUEBLER, Peter, DAVIS, John C, CHARLENE LIAO, X, LUBACH, Joseph W, DEESE, Alan, SOWELL, C. Gregory, CURRIE, Kevin S, YOUNG, Wendy B, KHOJASTEH, S. Cyrus, HOP, Cornelis E. C. A, SHIN, Young, WONG, Harvey, WONG, Susan, CORAGGIO, Melis, LA, Hank, BAUMGARDNER, Matthew, LE, Hoa, GOPAUL, Sashi, BOGGS, Jason

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Inhibitory Effects of Trapping Agents of Sulfur Drug Reactive Intermediates against Major Human Cytochrome P450 Isoforms by Sodhi, Jasleen K, Delarosa, Erlie Marie, Halladay, Jason S, Driscoll, James P, Mulder, Teresa, Dansette, Patrick M, Khojasteh, S Cyrus

“…In some cases, the formation of reactive species from the metabolism of xenobiotics has been linked to toxicity and therefore it is imperative to detect…”
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An ‘all-inclusive’ 96-well cytochrome P450 induction method: Measuring enzyme activity, mRNA levels, protein levels, and cytotoxicity from one well using cryopreserved human hepatocytes by Halladay, Jason S., Wong, Susan, Khojasteh, S. Cyrus, Grepper, Susan

“…The traditional in vitro approach for assessing potential CYP induction has been to simply compare changes in CYP activities using known CYP-specific probe…”
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The Effects of Drug Metabolizing Enzyme Inhibitors on Hepatic Efflux and Uptake Transporters by Cheong, Jonathan, Halladay, Jason S, Plise, Emile, Sodhi, Jasleen K, Salphati, Laurent

“…Non-selective chemical inhibitors of phase I and phase II enzymes are commonly used in in vitro metabolic studies to elucidate the biotransformation pathways…”
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On the prediction of hepatic clearance using the diluted plasma in metabolic stability assay by Berezhkovskiy, Leonid M, Khojasteh, S Cyrus, Halladay, Jason S, Hop, Cornelis E C A

“…It was suggested that in vivo hepatic clearance, CL(h), may be predicted rather accurately with the in vitro values of intrinsic clearance, CL(int), obtained…”
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Going Beyond Common Drug Metabolizing Enzymes: Case Studies of Biotransformation Involving Aldehyde Oxidase, γ-Glutamyl Transpeptidase, Cathepsin B, Flavin-Containing Monooxygenase, and ADP-Ribosyltransferase by Fan, Peter W, Zhang, Donglu, Halladay, Jason S, Driscoll, James P, Khojasteh, S Cyrus

“…The significant roles that cytochrome P450 (P450) and UDP-glucuronosyl transferase (UGT) enzymes play in drug discovery cannot be ignored, and these enzyme…”
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Discovery of an orally active benzoxaborole prodrug effective in the treatment of Chagas disease in non-human primates by Padilla, Angel M., Wang, Wei, Akama, Tsutomu, Carter, David S., Easom, Eric, Freund, Yvonne, Halladay, Jason S., Liu, Yang, Hamer, Sarah A., Hodo, Carolyn L., Wilkerson, Gregory K., Orr, Dylan, White, Brooke, George, Arlene, Shen, Huifeng, Jin, Yiru, Wang, Michael Zhuo, Tse, Susanna, Jacobs, Robert T., Tarleton, Rick L.

“…Trypanosoma cruzi , the agent of Chagas disease, probably infects tens of millions of people, primarily in Latin America, causing morbidity and mortality. The…”
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Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450 by Takahashi, Ryan H, Halladay, Jason S, Siu, Michael, Chen, Yuan, Hop, Cornelis E C A, Khojasteh, S Cyrus, Ma, Shuguang

“…GDC-0425 [5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile] is an orally bioavailable small-molecule inhibitor of checkpoint…”
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Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist by Wong, Harvey, Gould, Stephen E, Budha, Nageshwar, Darbonne, Walter C, Kadel, 3rd, Edward E, La, Hank, Alicke, Bruno, Halladay, Jason S, Erickson, Rebecca, Portera, Chia, Tolcher, Anthony W, Infante, Jeffery R, Mamounas, Michael, Flygare, John A, Hop, Cornelis E C A, Fairbrother, Wayne J

“…The application of modeling and simulation techniques is increasingly common in the preclinical stages of the drug development process. GDC-0917…”
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Consistency of the novel equations for determination of hepatic clearance and drug time course in liver that account for the difference in drug ionization in extracellular and intracellular tissue water by Berezhkovskiy, Leonid M, Liu, Ning, Halladay, Jason S

“…Intrinsic clearances of seven diverse compounds in rat liver microsomes were measured at intracellular pH 7.0 and extracellular pH 7.4. The obtained values…”
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1-Aminobenzotriazole coincubated with (S)-warfarin results in potent inactivation of CYP2C9 by Sodhi, Jasleen K, Ford, Kevin A, Mukadam, Sophie, Wong, Susan, Hop, Cornelis E C A, Khojasteh, S Cyrus, Halladay, Jason S

“…1-Aminobenzotriazole (ABT) is a nonselective, mechanism-based inactivator of cytochrome P450 (P450) and a useful tool compound to discern P450- from…”
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On the maintenance of hepatocyte intracellular pH 7.0 in the in-vitro metabolic stability assay by Berezhkovskiy, Leonid M., Wong, Susan, Halladay, Jason S.

“…The account of pH difference between hepatocytes (intracellular pH 7.0) and extracellular water (pH 7.4) leads to the novel equation for hepatic clearance…”
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Comparative Pharmacokinetic and Disposition Studies of [1-14C]1-Eicosanylcyclohexane, a Surrogate Mineral Hydrocarbon, in Female Fischer-344 and Sprague-Dawley Rats by HALLADAY, Jason S, MACKERER, Carl R, TWERDOK, Lorraine E, SIPES, I. Glenn

“…White oils or waxes [mineral hydrocarbons (MHCs)] with substantial levels of saturated hydrocarbons in the range of C18 to C32 have produced hepatic…”
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Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human by Salphati, Laurent, Pang, Jodie, Plise, Emile G., Chou, Bilin, Halladay, Jason S., Olivero, Alan G., Rudewicz, Patrick J., Tian, Qingping, Wong, Susan, Zhang, Xiaolin

“…The phosphatidylinositol 3-kinase (PI3K) pathway is a major determinant of cell cycling and proliferation. Its deregulation is associated with the development…”
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Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluorination by Driscoll, James P, Aliagas, Ignacio, Harris, Jennifer J, Halladay, Jason S, Khatib-Shahidi, Sheerin, Deese, Alan, Segraves, Nathaniel, Khojasteh-Bakht, S. Cyrus

“…Here, we report on the mechanism by which flavin-containing monooxygenase 1 (FMO1) mediates the formation of a reactive intermediate of…”
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Novel Mechanism for Dehalogenation and Glutathione Conjugation of Dihalogenated Anilines in Human Liver Microsomes: Evidence for ipso Glutathione Addition by Zhang, Chenghong, Kenny, Jane R, Le, Hoa, Deese, Alan, Ford, Kevin A, Lightning, Luke K, Fan, Peter W, Driscoll, James P, Halladay, Jason S, Hop, Cornelis E. C. A, Khojasteh, S. Cyrus

“…The objective of the present study was to investigate the influence of halogen position on the formation of reactive metabolites from dihalogenated anilines…”
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For a series of methylindole analogs, reactive metabolite formation is a poor predictor of intrinsic cytotoxicity in human hepatocytes by Zhang, Chenghong, Ma, Shuguang, Delarosa, Erlie Marie, Tay, Suzanne, Sodhi, Jasleen, Musinipally, Vivek, Chang, Patricia, Pai, Rama, Halladay, Jason S., Misner, Dinah, Kenny, Jane R., Hop, Cornelis E. C. A., Khojasteh, S. Cyrus

“…The formation of reactive metabolites (RMs) can lead to in vitrocytotoxicity, and, therefore, intrinsic cytotoxicity studies in human hepatocytes are often…”
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