New Perspectives in DMPK: Informing Drug Discovery


Programme - Monday, 10 February 2014

Drug Biotransformation and Reactive Metabolites

  • ADMET in 2014: still more exceptions than rules?
    Andy Pike
    Pfizer (UK) 
  • Understanding species and tissue-dependent differences in carboxylesterase-mediated metabolism
    Phil Butler
    Cyprotex Discovery Ltd (UK) 
  • Discovery DMPK in the rapidly evolving R&D sector
    Richard Weaver
    XenoGesis Ltd (UK) 
  • Interplay between enzymes and transporters in defining hepatic drug clearance and intracellular concentration of drugs
    Brian Houston
    University of Manchester (UK)
     

Toxicology / Omics

  • Contemporary medicinal chemistry of glucuronides
    Andrew Stachulski
    University of Liverpool (UK) 
  • Comparative metabonomic analysis of paracetamol (N-acetyl-p-aminophenol, APAP) hepatotoxicity and its non-toxic isomer N-acetyl-m-aminophenol (AMAP)
    Michael Kyriakides
    Imperial College London (UK) 
  • Forewarned is forearmed: development of pyrethroid activity based protein profiling probes (PyABPs) to predict insecticide resistance liabilities
    Mark Paine
    Liverpool School of Tropical Medicine (UK)
     

Programme - Tuesday, 11 February 2014

New Perspectives: Computational Approaches

  • Novel in vitro and in silico models of drug metabolism and toxicity
    Dominic Williams, MRC Centre for Drug Safety Science
    University of Liverpool (UK) 
  • Simulating individual variability in pharmacokinetics as a risk factor for drug toxicity
    Iain Gardner
    Simcyp (UK) 
  • Design, synthesis and biological evaluation of novel quinazoline derivatives with nitric oxide release moieties as preferential selective COX-II inhibitors
    Doaa Boshra Farag
    Misr International University (Egypt) 
  • Covalent inhibition – modelling and modulating compound reactivity and its exploitation on novel targets
    Nicola Colclough
    AstraZeneca Pharmaceuticals (UK) 
  • A UPLC-MS based study of the metabolism of tienilic acid and tienilic acid isomer
    Isobelle Grant
    Imperial College London (UK) 
  • Biological activities of Amazonian natural products
    Luis Kanzaki
    University of Brasilia (Brazil) 
  • Microbial metabolites and hepatic drug metabolism: a high throughput screen
    Glynn Martin
    University of Reading (UK) 
  • Physiologically based pharmacokinetic (PBPK) modeling and simulation: an application in the hit to lead stage
    Marisa Martinez-Martinez
    GlaxoSmithKline (Spain) 
  • High-throughput approach for metabolic stability screening in hepatocytes
    Astrid Milic
    Fidelta Ltd (Croatia) 
  • Probing the molecular targets of the endoperoxides: a proteomic approach
    Hanafy Mohamed
    University of Liverpool (UK) 
  • Drug transporters: role and importance in ADME and drug development
    Glynis Nicholls
    Independent Consultant (UK)
     

The Consequences: Drug Discovery and Development

  • Role of DMPK platform science and technologies in helping early discovery research
    Andy Harrell
    GlaxoSmithKline (UK)
  • Pharmacokinetics in drug discovery: where have we got to? how did we get here? where are we going?
    Peter Webborn
    AstraZeneca (UK) 
  • Role of zebrafish in drug discovery and development
    Mohammed Yaqoob
    Pharmidex (UK) 
  • CYP1A1 and CYP2W1 as cancer targets for duocarmycin bioprecursor development
    Klaus Pors
    Institute of Cancer Therapeutics, University of Bradford (UK) 
  • A novel methodology to measure the impact of active transport on intracellular unbound concentrations
    André Mateus
    Uppsala University (Sweden)
     

Keynote

  • Mitigation strategies for reactive intermediates in drug discovery
    Tom Baillie
    University of Washington (USA)
     

Downloadable Files

Interplay between enzymes and transporters in defining hepatic drug clearance and intracellular concentration of drugs
Brian Houston
PDF iconPDF (605k)  

Contemporary medicinal chemistry of glucuronides
Andrew Stachulski
PDF iconPDF (918k)  

Forewarned is forearmed: development of pyrethroid activity based protein profiling probes (PyABPs) to predict insecticide resistance liabilities
Mark Paine
PDF iconPDF (1199k)  

Novel in vitro and in silico models of drug metabolism and toxicity
Dominic Williams
PDF iconPDF (3264k)  

Simulating individual variability in pharmacokinetics as a risk factor for drug toxicity
Iain Gardner
PDF iconPDF (1641k)  

Design, synthesis and biological evaluation of novel quinazoline derivatives with nitric oxide release moieties as preferential selective COX-II inhibitors
Doaa Boshra Farag
PDF iconPDF (91k)  

A UPLC-MS based study of the metabolism of tienilic acid and tienilic acid isomer
Isobelle Grant
PDF iconPDF (58k)  

Biological activities of Amazonian natural products
Luis Kanzaki
PDF iconPDF (132k)  

Physiologically based pharmacokinetic (PBPK) modeling and simulation: an application in the hit to lead stage
Marisa Martinez-Martinez
PDF iconPDF (65k)  

High-throughput approach for metabolic stability screening in hepatocytes
Astrid Milic
PDF iconPDF (34k)  

Probing the molecular targets of the endoperoxides: a proteomic approach
Hanafy Mohamed
PDF iconPDF (44k)  

Drug transporters: role and importance in ADME and drug development
Glynis Nicholls
PDF iconPDF (37k)  

Role of DMPK platform science and technologies in helping early discovery research
Andy Harrell
PDF iconPDF (1063k)  

Pharmacokinetics in drug discovery: where have we got to? how did we get here? where are we going?
Peter Webborn
PDF iconPDF (606k)  

Mitigation strategies for reactive intermediates in drug discovery
Tom Baillie
PDF iconPDF (658k)  


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