Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier

Authors: Colclough, Nicola ^*, Alluri, Ravindra V., Tucker, James W., Gozalpour, Elnaz, Li, Danxi, Du, Hongwen, Li, Wei, Harlfinger, Stephanie, O’Neill, Daniel J., Sproat, Graham G., Chen, Kan, Yan, Yumei, McGinnity, Dermot F.

Source: In Drug Metabolism and Disposition February 2024 52(2):95-105

The Disconnect in Intrinsic Clearance Determined in Human Hepatocytes and Liver Microsomes Results from Divergent Cytochrome P450 Activities

Authors: Bapiro, Tashinga E. ^*, Martin, Scott ¹, Wilkinson, Stephen D., Orton, Alexandra L., Hariparsad, Niresh, Harlfinger, Stephanie, McGinnity, Dermot F. ^**

Source: In Drug Metabolism and Disposition July 2023 51(7):892-901

Challenges and Opportunities for Improved Drug–Drug Interaction Predictions for Renal OCT2 and MATE1/2‐K Transporters

Authors: Krishnan, Srinivasan, Ramsden, Diane, Ferguson, Douglas, Stahl, Simone H., Wang, Joanne, McGinnity, Dermot F., Hariparsad, Niresh

Source: Clinical pharmacology & therapeutics. 112(3):562-572

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100163862038.0x000001&indx=1&recIds=ETOCvdc_100163862038.0x000001

Current Practices, Gap Analysis, and Proposed Workflows for PBPK Modeling of Cytochrome P450 Induction: An Industry Perspective

Authors: Hariparsad, Niresh, Ramsden, Diane, Taskar, Kunal, Badée, Justine, Venkatakrishnan, Karthik, Reddy, Micaela B., Cabalu, Tamara, Mukherjee, Dwaipayan, Rehmel, Jessica, Bolleddula, Jayaprakasam, Emami Riedmaier, Arian, Prakash, Chandra, Chanteux, Hugues, Mao, Jialin, Umehara, Kenichi, Shah, Kushal, De Zwart, Loeckie, Dowty, Martin, Kotsuma, Masakatsu, Li, Mengyao, Pilla Reddy, Venkatesh, McGinnity, Dermot F., Parrott, Neil

Source: Clinical pharmacology & therapeutics. 112(4):770-781

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100160568462.0x000001&indx=1&recIds=ETOCvdc_100160568462.0x000001

Evaluation of the Disconnect between Hepatocyte and Microsome Intrinsic Clearance and In Vitro In Vivo Extrapolation Performance

Authors: Williamson, Beth ^*, Harlfinger, Stephanie, McGinnity, Dermot F.

Source: In Drug Metabolism and Disposition November 2020 48(11):1137-1146

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

Authors: Pike, Andy, Williamson, Beth, Harlfinger, Stephanie, Martin, Scott, McGinnity, Dermot F.

Source: In Drug Discovery Today October 2020 25(10):1793-1800

Improving the Accuracy of Predicted Human Pharmacokinetics: Lessons Learned from the AstraZeneca Drug Pipeline Over Two Decades

Authors: Davies, Michael, Jones, Rhys D.O., Grime, Ken, Jansson-Löfmark, Rasmus, Fretland, Adrian J., Winiwarter, Susanne, Morgan, Paul, McGinnity, Dermot F.

Source: In Trends in Pharmacological Sciences June 2020 41(6):390-408

Building on the success of osimertinib: achieving CNS exposure in oncology drug discovery

Authors: Colclough, Nicola, Chen, Kan, Johnström, Peter, Fridén, Markus, McGinnity, Dermot F.

Source: In Drug Discovery Today May 2019 24(5):1067-1073

Epoxidation of Olefins by Cytochrome P450: Evidence from Site-Specific Mutagenesis for Hydroperoxo-Iron as an Electrophilic Oxidant

Authors: McGinnity, Dermot F., Coon, Minor J.

Source: Proceedings of the National Academy of Sciences of the United States of America, 1998 Mar . 95(7), 3555-3560.

Access URL: https://www.jstor.org/stable/44521

A PKPD Case Study: Achieving Clinically Relevant Exposures of AZD5991 in Oncology Mouse Models.

Authors: White, Michael J., Cheatham, Letitia, Wen, Shenghua, Scarfe, Graeme, Cidado, Justin, Reimer, Corinne, Hariparsad, Niresh, Jones, Rhys D. O., Drew, Lisa, McGinnity, Dermot F., Vasalou, Christina

Source: AAPS Journal; Jul2023, Vol. 25 Issue 4, p1-8, 8p

Prediction of Human Renal Clearance from Preclinical Species for a Diverse Set of Drugs That Exhibit Both Active Secretion and Net Reabsorption

Authors: Paine, Stuart W. ^*, Ménochet, Karelle, Denton, Rebecca, McGinnity, Dermot F., Riley, Robert J.

Source: In Drug Metabolism and Disposition June 2011 39(6):1008-1013

Interspecies evaluation of a physiologically based pharmacokinetic model to predict the biodistribution dynamics of dendritic nanoparticles.

Authors: Vasalou, Christina, Harding, Joanna, Jones, Rhys D. O., Hariparsad, Niresh, McGinnity, Dermot F.

Source: PLoS ONE; 5/17/2023, Vol. 18 Issue 5, p1-22, 22p

Subject Terms: RATS, MICE, PHARMACOKINETICS, NANOPARTICLES, SENSITIVITY analysis, DOGS, ALLOMETRY

Evaluation of Multiple in Vitro Systems for Assessment of CYP3A4 Induction in Drug Discovery: Human Hepatocytes, Pregnane X Receptor Reporter Gene, and Fa2N-4 and HepaRG Cells

Authors: McGinnity, Dermot F. ^*, Zhang, George, Kenny, Jane R. ¹, Hamilton, Geraldine A., Otmani, Sara, Stams, Karen R., Haney, Suzzette, Brassil, Patrick, Stresser, David M., Riley, Robert J.

Source: In Drug Metabolism and Disposition June 2009 37(6):1259-1268

Integrated in Vitro Analysis for the in Vivo Prediction of Cytochrome P450-Mediated Drug-Drug Interactions

Authors: McGinnity, Dermot F. ^*, Waters, Nigel J. ¹, Tucker, James, Riley, Robert J.

Source: In Drug Metabolism and Disposition June 2008 36(6):1126-1134

The pivotal role of hepatocytes in drug discovery

Authors: Soars, Matthew G., McGinnity, Dermot F., Grime, Ken, Riley, Robert J.

Source: In Chemico-Biological Interactions 2007 168(1):2-15

EVALUATION OF TIME-DEPENDENT CYTOCHROME P450 INHIBITION USING CULTURED HUMAN HEPATOCYTES

Authors: McGinnity, Dermot F. ^*, Berry, Amanda J., Kenny, Jane R., Grime, Ken, Riley, Robert J.

Source: In Drug Metabolism and Disposition August 2006 34(8):1291-1300

Quantitative Evaluation of Dendritic Nanoparticles in Mice: Biodistribution Dynamics and Downstream Tumor Efficacy Outcomes.

Authors: Vasalou, Christina, Ferguson, Douglas, Weimin Li, Muse, Victorine, Gibbons, Francis D., Sonzini, Silvia, Guangnong Zhang, Pop-Damkov, Petar, Gangl, Eric, Balachander, Srividya B., Shenghua Wen, Schuller, Alwin G., Puri, Sanyogitta, Mazza, Mariarosa, Ashford, Marianne, Fretland, Adrian J., McGinnity, Dermot F., Jones, Rhys D. O.

Source: Molecular Pharmaceutics; 1/3/2022, Vol. 19 Issue 1, p172-187, 16p

Epoxidation of olefins by cytochrome P450: evidence from site-specific mutagenesis for hydroperoxo-iron as an electrophilic oxidant.

Authors: Vaz, Alfin D. N., McGinnity, Dermot F., Coon, Minor J.

Source: Proceedings of the National Academy of Sciences of the United States of America; March 31 1998, Vol. 95 Issue 7, p3555-3560, 6p

Mechanistic physiology-based pharmacokinetic modeling to elucidate vincristine-induced peripheral neuropathy following treatment with novel kinase inhibitors.

Authors: Pilla Reddy, Venkatesh, Fretland, Adrian J., Zhou, Diansong, Sharma, Shringi, Chen, Buyun, Vishwanathan, Karthick, McGinnity, Dermot F., Xu, Yan, Ware, Joseph A.

Source: Cancer Chemotherapy & Pharmacology; Sep2021, Vol. 88 Issue 3, p451-464, 14p

Subject Terms: PERIPHERAL neuropathy, KINASE inhibitors, ANTINEOPLASTIC combined chemotherapy protocols, DRUG interactions, PHARMACOKINETICS, P-glycoprotein, RITUXIMAB

Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist

Authors: Scott, James S., Moss, Thomas A., Balazs, Amber, Barlaam, Bernard, Breed, Jason, Carbajo, Rodrigo J., Chiarparin, Elisabetta, Davey, Paul R. J., Delpuech, Oona, Fawell, Stephen, Fisher, David I., Gagrica, Sladjana, Gangl, Eric T., Grebe, Tyler, Greenwood, Ryan D., Hande, Sudhir, Hatoum-Mokdad, Holia, Herlihy, Kara, Hughes, Samantha, Hunt, Thomas A., Huynh, Hoan, Janbon, Sophie L. M., Johnson, Tony, Kavanagh, Stefan, Klinowska, Teresa, Lawson, Mandy, Lister, Andrew S., Marden, Stacey, McGinnity, Dermot F., Morrow, Christopher J., Nissink, J. Willem M., O’Donovan, Daniel H., Peng, Bo, Polanski, Radoslaw, Stead, Darren S., Stokes, Stephen, Thakur, Kumar, Throner, Scott R., Tucker, Michael J., Varnes, Jeffrey, Wang, Haixia, Wilson, David M., Wu, Dedong, Wu, Ye, Yang, Bin, Yang, Wenzhan

Source: Journal of Medicinal Chemistry; December 2020, Vol. 63 Issue: 23 p14530-14559, 30p