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SMi Presents their 6th annual conference on...

ADMET: 

Translating Research into Clinical Outcomes

About the conference

 

ADMET performs a vital function in early drug discovery, without this screening the proportion of formulations failing at the trails stage of drug development would rise, and the financial implications would be severe. Therefore, it is crucial that the ADMET programmes that companies employ to filter their drug candidates down are as thorough as possible, and up to date with the latest technology.


This conference will address a wide range of in vivo, in silico and in vitro ADMET case studies in a showcase of examples from an internationally renowned line up of speakers with intimate knowledge of the latest industry developments.   

 

View the Programme | Register Your Place |

Key Topics addressed:

 

  • Metabonomics
  • Optimisation and prediction
  • Toxicity and genotoxicity
  • Blood brain barrier and bioavailability
  • In silico, in vitro and in vivo correlations
  • PK/PD modeling
  • Proteomics
  • Regulatory developments

 

 

Interested in speaking at the conference?  Contact the Conference Producer.

For sponsorship and exhibition opportunities, Contact our Sponsorship Department.

 RNAi 3

Make sure you save the date for our half day pre-conference workshop

Associated with the conference there will be a half-day interactive workshop on "Predictive Toxicology Model Building", taking place on Tuesday 5th of June.

The workshop aims to provide a set of stimulating problem-solving activities used latest advanced modelling and analysis techniques and case studies of relevance to research scientists, modellers, and risk assessors, needing to predict the toxicities of compounds. Workshop participants will study problems with hands-on examples using leading methods and discuss complex issues highlighted by examples presented by the instructor.

Leading this workshop will be Barry Hardy, Director, Douglas Connect To see more information about the workshop, please see the comprehensive workshop page

Workshop hosted by: 

 

 

 

Our expert speaker line up:

Mathieu Vinken, Pharm.D. Department of Toxicology,  Vrije Universiteit Brussels
Willem Schoonen
Senior Research Scientist Toxicology & Drug Disposition MSD
Mike Piper
Senior Business Development Manager CXR Biosciences
Alan Wilson,
Vice President, Drug Metabolism, Pharmacokinetics, Toxicology and Pathology, Lexicon Pharmaceuticals
Alexander Alex
, Computational Chemistry, Pfizer
Frederick Tam
, Senior Clinical Lecturer/Hon. Consultant Nephrologist, Imperial College London
Helga Gerets
, Senior Scientist, In Vitro Toxicology UCB Pharma

Vijay Gombar, Research Advisor, Drug Disposition, Eli Lilly  
Vibeke Sunesen, Pharmacokineticist, Preclinical Development, LEO Pharma
Dieter Deforce
, Professor, Laboratory of Pharmaceutical Biotechnology University of Gent
Richard Weaver
Associate Principal Scientist AstraZeneca
Aileta Prabhu
, Senior Scientist/Group Leader, PKPDS, Development Sciences, Genentech
Dolo Diaz,
Investigative Safety Assessment, Genentech
Balazs Sarkadi,
Membrane Research Group, Hungarian Academy of Sciences.
Gergely Szakacs
, Senior Research Fellow at the Institute of Enzymology, Hungarian Academy of Sciences
Dieter Deforce,
Professor, Laboratory of Pharmaceutical Biotechnology University of Gent
Pablo Morentin Gutierrez
, Associate Principal Scientist, DMPK-IM, AstraZeneca
John Comer
, Technical Director, Sirius Analytical
Andrew Brown,
Senior Scientific Investigator, GlaxoSmithKline
David Buckley,
Principal Scientist, XenoTech
Janice Yau Yi Lau
Senior Group Leader Drug Metabolism Abbott

Katya Tsaioun Chief Scientific Officer Cyprotex Discovery

 

CSOs, CMOs, Vice Presidents, Presidents, Heads, Directors, Team Leaders, and Senior Scientists from the following roles:

 

  • Drug Discovery
  • Preclinical Development
  • ADME
  • DMPK
  • Pharmacokinetics
  • Toxicology / metabolism
  • Computational Chemistry
  • Molecular Modelling
  • Structural Biologists
  • Biomolecular Screening
  • Medicinal Chemistry
  • Screening and Lead Characterisation
  • Drug Design
  • Physical Chemistry

 

     

 

Conference programme

8:30 Registration & Coffee

9:00 Chairman's Opening Remarks

Richard Weaver

Richard Weaver, Associate Principal Scientist, AstraZeneca

9:10 Cell culture and in vivo model to develop new treatments for renal diseases

Frederick W K Tam

Frederick W K Tam, Senior Clinical Lecturer (Renal Medicine), Imperial College London West London Renal and Transplant Centre Hammersmith Hospital

  • Cytokines in pathogenesis of renal diseases
  • Cell culture model
  • In vivo model (progression from inflammation to fibrosis and renal failure)
  • Assessing the effect of small molecule inhibitors in vitro and in vivo
  • Translation to clinical practice
  • 9:45 Applications of humanized mouse models in evaluation of drug-drug interactions, pathways of metabolism and drug safety

    Mike Piper

    Mike Piper, Senior Business Development Manager, CXR Biosciences

  • Current preclinical models can be poorly predictive of DMPK and Safety in humans, due to profound interspecies differences in key pathways of metabolism
  • We will present data in mice humanised for cytochrome P450s, nuclear receptors and drug transporters, demonstrating that these mice are more predictive of man
  • Case studies including quantitative prediction of inducers on the AUC of victim substrates in man, production of human disproportionate metabolites in a mouse model, & species-specific inhibition effects
  • 10:20 Morning Coffee

    10:45 Selection of preclinical species with a focus on the minipig

    Vibeke Sunesen

    Vibeke Sunesen, Pharmacokineticist, Preclinical Development, Leo Pharma

  • Can ADMET properties be adequately predicted?
  • Pros and cons when using the minipig
  • Case studies: we used the minipig
  • 11:20 Using measured physicochemical properties as an aid to early candidate selection

    John Comer

    John Comer, Co-founder & Technical Director, Sirius Analytical Instruments

  • Measured values bring increased confidence to ADME studies
  • Fast methods for pKa and solubility measurement
  • Small-scale dissolution studies help prepare for effective pre-formulation
  • 11:55 Where does PKPD add value in drug discovery?

    Pablo Morentin-Gutierrez

    Pablo Morentin-Gutierrez, Associate Principal Scientist , AstraZeneca

  • Integration of PK/PD in Lead Identification and Lead Optimization phases
  • Influencing Phase I trials using preclinical PK/PD knowledge
  • Overcoming major hurdles to implement PK/PD reasoning in Drug Discovery
  • 12:30 Networking Lunch

    13:30 ADMET and PK/PD modelling in drug discovery and development - New horizons and applications

    Alan Wilson

    Alan Wilson, Drug Metabolism, Pharmacokinetics, Toxicology and Pathology, Lexicon Pharmaceuticals Inc

  • Role of ADMET in optimizing drug discovery and development
  • Strategies, approaches and applications
  • Incorporating early formulation and PK/PD Modelling
  • Future directions, opportunities and challenges
  • 14:05 Application of in silico methods in the prediction of ADME

    Alexander Alex

    Alexander Alex, Director, Computational Chemistry, Pfizer

  • Molecular properties in drug discovery.
  • Application of in silico ADMET in drug design.
  • Case study for prediction of drug metabolism.
  • Rationalisation and prediction of drug absorption
  • 14:40 The influence of DMPK & physicochemical science to all key discovery disciplines

    Richard Weaver

    Richard Weaver, Associate Principal Scientist, AstraZeneca

  • It’s all in the structure
  • Prediction of human pharmacokinetics and dose
  • DMPK is an integral partner in drug discovery 
  • 15:15 Afternoon Tea

    15:45 Relationships between physicochemical properties and ADMET

    Janice Yau Yi Lau

    Janice Yau Yi Lau, Group Leader, Abbott Laboratories

  • cLog P/Log D are the top most important physicochemical properties that not only affect ADME properties but also safety outcomes.
  • Physicochemical properties are important determinant of CNS penetration
  • Solubility and permeability decrease with increase in MW, cLog P and PSA and is important for absorption and can increase oral bioavailability
  • Protein binding increases with increase in MW, cLog P, and PSA which affect clearance and efficacy
  • 16:20 Brain Tissue Binding of Drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high -throughput method

    Kathleen Boehme

    Kathleen Boehme, Study Director, Sovicell

  • Estimating the unbound fraction of drugs in brain as essential for the evaluation and interpretation of the pharmacokinetics and pharmacodynamics of new central nervous system drug candidates.
  • The low throughput downside of Dialysis-based methods
  • Combining the TRANSIL brain absorption assay with liquid chromatography mass spectrometry.
  • Comparing free fractions fu,brain obtained using the TRANSIL brain absorption assay and equilibrium dialysis methods for a test set of 65 drugs (27 marketed and 38 GlaxoSmithKline proprietary drugs).
  • This not only significantly reduces the biological matrix required but also increases the throughput as compared to the conventional dialysis methods
  • 16:55 CNS delivery of antibodies, are we there yet?

    Saileta Prabhu

    Saileta Prabhu, Senior Scientist, PKPDS Development Sciences, Genetech

    Overview of the transport barriers for antibodies in the brain including the blood-brain barrier (BBB)
    Disposition of antibodies in the CNS with focus on influx and efflux pathways
    BBB physiological parameters in neurodegenerative disease mouse models, and its potential impact on drug delivery
    Transporting therapeutic antibodies to the brain by receptor-mediated transcytosis
    Challenges in CNS delivery of antibodies to patients

    17:30 Assessment of Human Pharmacokinetics from QSAR Models: Best Model for Humans is Human

    Vijay Gombar

    Vijay Gombar, Research Advisor, Eli Lilly & Co

    • Presentation will focus on development and performance of QSAR models for human intravenous clearance and volume of distribution
    • QSAR predictions are compared with experimental data for a simulated test set of 235 drugs
    • When tested on 109 randomly selected drugs, the VDss in silico model predicted 50% and 90% compounds within 1.6-fold and 4.9-fold deviation from VDss measured in clinical studies 
    • Through an analysis of comparison between experimental data and predictions for proprietary compounds, limits of application of models are identified

    18:00 Chairman’s Closing Remarks and Close of Day One

    Richard Weaver

    Richard Weaver, Associate Principal Scientist, AstraZeneca

    8:30 Registration & Coffee

    9:00 Morning Chairman's Opening Remarks

    Balazs Sarkadi

    Balazs Sarkadi, Head, Membrane Biology Research Group, Hungarian Academy of Sciences

    9:10 Pre-clinical screening of anti-HER2 Nanobodies for molecular imaging of breast cancer

    Nick Devoogdt

    Nick Devoogdt, Cellular and Molecular Immunology, Vrije Universiteit Brussel

  • Evaluating HER2 expression in vivo by radioimmunodetection using Nanobodies and single photon emission computed tomography (SPECT)
  • The potential of 99mTc-Nanobodies produced against HER2 as tracers for non-invasive imaging of HER2 expression
  • Study details
  • One 99mTc-Nanobody identified as the lead compound for a phase I clinical study
  • 9:45 Targeted and non-targeted proteomics in biomarker research

    Dieter Deforce

    Dieter Deforce, Professor, Gent University

  • Targeted and non-targeted proteomics in biomarker research.
  • Different technological platforms for non-targeted and targeted proteome analysis
  • Identification of biomarkers
  • Qualification of biomarkers
  • Biomarkers in ADMET
  • 10:20 Morning Coffee

    10:50 Metabolites as perpetrators of drug interactions

    David Buckley

    David Buckley, Principal Scientist, XenoTech

  • Formation of metabolites that inhibit drug-metabolizing enzymes and drug transporters
  • Regulatory guidance on metabolites and current in vitro techniques
  • Clinical significance of metabolites as inhibitors of CYP enzymes and transporters
  • 11:25 Is Nrf2 a good biomarker of oxidative stress and reactive metabolites?

    Helga Gerets

    Helga Gerets, Senior Scientist, In Vitro Toxicology, UCB

  • Introduction on Nrf2: its role, pathway and activation
  • Models/experiments used to investigate toxicities related to reactive metabolites/oxidative stress
  • Experimental approach 1: Cellular toxicogenomic analysis and potential biomarkers
  • Experimental approach 2: AREc32 cell line: predictivity, advantage and limitations
  • Relationship between hepatotoxicity and reactive metabolites
  • 12:00 The chemoimmunity concept as a framework to understand ADME-Tox

    Balazs Sarkadi

    Balazs Sarkadi, Head, Membrane Biology Research Group, Hungarian Academy of Sciences

  • ABC “efflux” transporters involved in the fate of drugs,
  • “Uptake” transporters involved in the fate of drugs,
  • Interactions between transporters and enzymes of drug metabolism,
  • Common regulatory pathways for transporters and metabolic enzymes,
  • A systems biology approach to analyze drug and xenobiotic interactions within the frame of the chemoimmunity network concept
  • 12:35 Networking Lunch

    13:35 Afternoon Chair's Opening Remarks

    Dolo Diaz

    Dolo Diaz, Investigative Safety Assessment, Genetech

    13:45 State-of-the-art overview of strategies used for the establishment of liver-based in vitro systems for long-term pharmaco-toxicological testing

    Mathieu Vinken

    Mathieu Vinken, Department of Toxicology, Vrije Universiteit Brussel

  • Increasing importance of in vitro testing platforms for pharmaco-toxicological testing of new chemical entities
  • Overview of currently available primary hepatocyte culture systems and their shortcomings
  • Conventional and novel strategies to optimize primary hepatocyte cultures
  • Future directions
  • 14:20 Validation of CellCiphrTM Technology. Building on Experience of In Vitro Liver Cell Toxicity to Predict In Vivo DILI

    Katya Tsaioun

    Katya Tsaioun, Chief Scientific Officer , Cyprotex

    Thomas, Simon1; Metcalfe, Paul1;Tsaioun, Katya1,2
    1. Cyprotex, Macclesfield, SK10 2DR, United Kingdom.
    2. Apredica, Watertown, MA, United States

  • Toxicity is a key reason for drug attrition.
  • High Content Screening (HCS) allows early detection of indicators of cellular toxicity, covering a wide spectrum of cytopathological changes.
  • CellCiphr™ combines HCS with an proprietary ranking and classifying system for predicting in vivo toxicity.
  • CellCiphr™ also includes a set of proprietary in silico models for predicting the risk of compound failure in safety studies.
  • Here relative toxicity rankings of a selection of results for different cell models will be presented and discused.
  • Case studies of CellCiphr™ use in derisking pharmaceutical programs will be presented.
  • 14:55 Afternoon Tea

    15:25 Toxicogenomics within the pharmaceutical industry

    Willem Schoonen

    Willem Schoonen, Senior Research Scientist, MSD

  • The focus is on in vivo and in vitro liver toxicogenomics
  • Prediction scores for in vivo rat liver toxicity with ToxShield
  • Prediction scores for in vitro rat precision-cut liver slice toxicity with ToxShield
  • Segregation of gene sets for genotoxicity in human liver HepG2 hepatocytes
  • Development of luciferase reporter based HepG2 cells for genotoxicity
  • 16:00 The Prozac paradox – predicting clinical toxicity from in vitro assays

    Andrew Brown

    Andrew Brown, Investigator, GlaxoSmithKline

  • How to interpret in vitro toxicity data in early drug discovery
  • Relating in vitro toxicity to physicochemical properties and the concept of compound “promiscuity”
  • New frontiers: Non-functional cardiotoxicity and other non-liver tissue toxicity
  • 16:35 Pharmacokinetic drivers of toxicity for small molecules: Evaluating plasma-tissue concentration relationships

    Dolo Diaz

    Dolo Diaz, Investigative Safety Assessment, Genetech

  • Tissue drug exposures versus drug exposures in the interpretation of toxicity data
  • Improved In vitro-in vivo correlations and the understanding of in vivo toxicities considering target organ exposures.   
  • Approximate prediction of tissue drug levels using the volume of distribution (Vss) and the clearance (CLp) of a particular molecule
  • Physicochemical drivers of tissue distribution and how they can affect safety margins
  • 17:10 Chairman’s Closing Remarks and Close of Day Two

    +

    Workshops

    Predictive Toxicology Model Building
    Workshop

    Predictive Toxicology Model Building

    Copthorne Tara Hotel
    5th July 2011
    London, United Kingdom

    Copthorne Tara Hotel

    Scarsdale Place
    Kensington
    London W8 5SR
    United Kingdom

    Copthorne Tara Hotel

    The Copthorne Tara Hotel London Kensington is an elegant contemporary four-star hotel in prestigious Kensington, located just a two minutes walk from High Street Kensington underground station, making exploring easy. The hotel offers well-appointed and comfortable guest rooms combining Standard, Superior and Club accommodation. Club rooms offer iconic views over the city and include Club Lounge access for complimentary breakfast and refreshments. Guests can sample the authentic Singaporean, Malaysian and Chinese cuisine at Bugis Street, traditional pub fare at the Brasserie Restaurant & Bar or relax with a delicious drink at West8 Cocktail Lounge & Bar.

    The Copthorne Tara Hotel boasts 745 square meters of flexible meeting space, consisting of the Shannon Suite and the Liffey Suite, ideal for hosting conferences, weddings and social events. Facilities include access to the business centre 24 hours a day, fully equipped fitness room, gift shop, theatre desk and Bureau de Change. With ample onsite parking outside the London congestion charge zone and excellent transport links via Heathrow Airport, the hotel is the perfect location for business or leisure stays. The hotel is within close proximity to the shops of High Street Kensington, Knightsbridge and Westfield London, Olympia Conference Centre, Royal Albert Hall, Kensington Palace and Hyde Park.

     

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