D F McGinnity

Summary

Affiliation: AstraZeneca R and D

Publications

  1. ncbi The pivotal role of hepatocytes in drug discovery
    Matthew G Soars
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, Leicestershire LE11 5RH, UK
    Chem Biol Interact 168:2-15. 2007
  2. ncbi Evaluation of human pharmacokinetics, therapeutic dose and exposure predictions using marketed oral drugs
    D F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, UK
    Curr Drug Metab 8:463-79. 2007
  3. ncbi 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
    Dermot F McGinnity
    Discovery DMPK, AstraZeneca Research and Development, Charnwood, UK
    Drug Metab Dispos 37:1259-68. 2009
  4. ncbi Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 32:1247-53. 2004
  5. ncbi Prediction of CYP2C9-mediated drug-drug interactions: a comparison using data from recombinant enzymes and human hepatocytes
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 33:1700-7. 2005
  6. ncbi Evaluation of time-dependent cytochrome P450 inhibition using cultured human hepatocytes
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 34:1291-300. 2006
  7. ncbi Integrated in vitro analysis for the in vivo prediction of cytochrome P450-mediated drug-drug interactions
    Dermot F McGinnity
    Discovery Drug Metabolism and Pharmacokinetics, AstraZeneca R and D Charnwood, Loughborough, Leicestershire, United Kingdom
    Drug Metab Dispos 36:1126-34. 2008
  8. ncbi Efficient assessment of the utility of immortalized Fa2N-4 cells for cytochrome P450 (CYP) induction studies using multiplex quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR) and substrate cassette methodologies
    J R Kenny
    AstraZeneca R and D Charnwood, Loughborough, UK
    Xenobiotica 38:1500-17. 2008
  9. ncbi A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes
    Robert J Riley
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 33:1304-11. 2005
  10. ncbi Predicting drug pharmacokinetics in humans from in vitro metabolism studies
    D F McGinnity
    Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough LE11 5RH, U K
    Biochem Soc Trans 29:135-9. 2001

Detail Information

Publications11

  1. ncbi The pivotal role of hepatocytes in drug discovery
    Matthew G Soars
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, Leicestershire LE11 5RH, UK
    Chem Biol Interact 168:2-15. 2007
    ..The study of hepatic uptake using isolated hepatocytes and the interplay between drug transport and metabolism with respect to both clearance and DDIs and subsequent IVIVE is also considered...
  2. ncbi Evaluation of human pharmacokinetics, therapeutic dose and exposure predictions using marketed oral drugs
    D F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, UK
    Curr Drug Metab 8:463-79. 2007
    ..The benefits and limitations of this holistic approach to PK and dose prediction within the drug discovery process are exemplified and discussed...
  3. ncbi 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
    Dermot F McGinnity
    Discovery DMPK, AstraZeneca Research and Development, Charnwood, UK
    Drug Metab Dispos 37:1259-68. 2009
    ..HepaRG cells are a valuable recent addition to the armory of in vitro tools for assessing CYP3A4 induction and seem to be an excellent surrogate of primary cells...
  4. ncbi Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 32:1247-53. 2004
    ....
  5. ncbi Prediction of CYP2C9-mediated drug-drug interactions: a comparison using data from recombinant enzymes and human hepatocytes
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 33:1700-7. 2005
    ....
  6. ncbi Evaluation of time-dependent cytochrome P450 inhibition using cultured human hepatocytes
    Dermot F McGinnity
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 34:1291-300. 2006
    ..Therefore, in addition to enzyme activity, mRNA and/or protein levels should be measured to fully evaluate the P450 induction potential of a drug candidate...
  7. ncbi Integrated in vitro analysis for the in vivo prediction of cytochrome P450-mediated drug-drug interactions
    Dermot F McGinnity
    Discovery Drug Metabolism and Pharmacokinetics, AstraZeneca R and D Charnwood, Loughborough, Leicestershire, United Kingdom
    Drug Metab Dispos 36:1126-34. 2008
    ....
  8. ncbi Efficient assessment of the utility of immortalized Fa2N-4 cells for cytochrome P450 (CYP) induction studies using multiplex quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR) and substrate cassette methodologies
    J R Kenny
    AstraZeneca R and D Charnwood, Loughborough, UK
    Xenobiotica 38:1500-17. 2008
    ..The sensitive and selective methodologies presented in this paper afford maximal data generation and enhanced throughput capability and are readily transferable to primary human hepatocytes or alternate cellular systems...
  9. ncbi A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes
    Robert J Riley
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK
    Drug Metab Dispos 33:1304-11. 2005
    ..The direct use of this model using only in vitro human data to predict the metabolic component of CL(h) is attractive, as it does not require extra information from preclinical studies in animals...
  10. ncbi Predicting drug pharmacokinetics in humans from in vitro metabolism studies
    D F McGinnity
    Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough LE11 5RH, U K
    Biochem Soc Trans 29:135-9. 2001
    ..001) and acids (r(2)=0.79, P<0.001) that may allow prediction of this property. Our laboratory has shown that recombinant enzymes are suitable for "frontline" predictive human metabolism studies in early drug discovery...
  11. ncbi From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis
    Brian Springthorpe
    AstraZeneca R and D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK
    Bioorg Med Chem Lett 17:6013-8. 2007
    ..The leading compound, 17 (AZD6140), is currently in a large phase III clinical trial for the treatment of acute coronary syndromes and prevention of thromboembolic clinical sequelae...