Topics of the MipTec Conference 2008
1. Drug Discovery Technologies
2. Biological Space: Targets and Tools
3. Chemical Space: Maximizing Compound Value
4. Early Safety Evaluation
5. Pharmacodynamics / Biomarkers
6. Structural and Computational Drug Discovery
1. Drug Discovery Technologies
Chairs
Christof Fattinger, Hoffmann-La Roche, CH
Al Kolb, KeyTech Solutions, US
Lorenz Mayr, Novartis, CH
Improvements in technologies have always been key to meeting the changing and challenging goals of drug discovery. This session has grown and adapted to these changing needs. The focus on automation and homogeneous luminescence and fluorescence-based methods has shifted to nanotechnologies for molecular interaction analysis and label-free assay methods. The importance of cell-based assays resulted in the inclusion of sessions on high-content screening and imaging. New concepts, early stage technologies and improvements to established methods will be presented. Please join us in the “Drug Discovery Technologies” session to learn about new trends and developments in technology and how they are being used to improve drug discovery. We will cover recent developments such as:
- Novel assay technologies
- Label-free detection methods
- High-content screening and imaging
- Stem & primary cells in drug discovery
- Cutting-edge technologies
2. Biological Space: Targets and Tools
Chairs
Thilo Enderle, Hoffmann-La Roche, CH
Hubert Haag, Sanofi Aventis, DE
Keith Wood, Promega, US
Biological aspects moved back into the spotlight of drug discovery. The proper assessment of novel targets, the choice of meaningful biological systems for predictive in-vitro assays and finally the sensitive visualization of biological processes are crucial for success. This session stresses the biological relevance of targets and screening concepts.
The presentations will cover advances in target identification and validation, pathway mapping and the impact of research tools such as RNAi. Trends in cell-based screening, like the use of primary cells or the application of sophisticated imaging assays, will be illustrated. Cutting edge biology tools and methods having impact on other technologies such as high content screening will be highlighted. Recently, the research tools also found their way into the product portfolios. Innovative approaches for future medicines will be discussed such as therapeutics proteins, RNAi and aptamers.
3. Chemical Space: Maximizing Compound Value
Chairs
Chris Lipinski, Melior Discovery, US
Dennis France, ArQule Inc., US
Ian Yates, Agilent, US
The value of an HTS screen has always been dependent on the chemistry design quality of the underlying screening library and on the quality of the infrastructure for the formatting, storage and distribution of the samples in the screening library. Much recent attention has focused on case histories of compound management efforts in the smaller, more resource-constrained organizations. There still continues to be debate on the ideal characteristics of a screening library with active involvement of computational chemists and medicinal chemists. The scope of screening libraries now encompasses a much broader range of chemistries. These issues of chemistry quality have become even more important with the increasing involvement of academic and smaller biotechnology companies in drug discovery and on the analytical side with the recognition that actual screening concentration may deviate significantly from the nominal concentration expected from dilution of DMSO stock solutions. The issue of chemistry false positives arising from flawed chemistry in the screening collection continues to be an area of concern. We will cover developments such as:
- Improving compound management infrastructure
- Advances in analytical quality of compound libraries
- Advances in design of screening libraries
- Understanding the cause of chemistry false positives
Chairs
Wolfgang Sauer, Merck Serono, CH
Mel Reichman, Lankenau Chemical Genomics Center, US
Anna Seelig, Biozentrum, University of Basel, CH
Emerging ADMET Technologies: From Program Project Concept to Phase IV Safety Monitoring
The pharmacological basis of therapeutics is comprised of two overarching scientific disciplines: pharmacodynamics and pharmacokinetics. It is often summarily stated: “pharmacodynamics is the study of what a drug does to the body; whereas pharmacokinetics is the study of what the body does to a drug”. The latter studies the absorption, distribution, metabolism, excretion and toxicology (ADMET) of drugs. Our distinguished speakers this year at MipTec provide an experts' survey of Experimental and Computational ADMET across the entire terrain of a modern Pharma enterprise.
Session Topics will include:
- Integration of High Throughput ADMET Throughout Discovery Research
- Earliest ADMET: State of the Art in Computational Technologies
- The Good, the Bad and the Ugly: Compound Killers vs. Killer Compounds
- Rapid Evolution Under Regulatory Selection: Biomarkers and Pharmacogenomics
- Regulatory Milieus for Safety Assessment and Post-Approval Monitoring
- Catastrophic Milestones in Pharmaceutical R&D
5. Pharmacodynamics / Biomarkers
Chairs
Roy Goodacre, University of Manchester, UK
Eric Bertrand, Novartis, CH
Christof Fattinger, Hoffmann-La Roche, CH
Biomarker discovery is important as it can help stratify patients and aid in drug development. There is thus intense interest in integrating biomarkers into the drug discovery and development process from the earliest stages on. The challenge of applying molecular profiling technologies to preclinical and clinical environments are currently being met through technological, computational and conceptual advances.
Progresses in analytical technologies are improving rapidly as are the accuracy and reliability of profiling technologies in order to deal with the variability inherent to complex organisms. Another exciting trend is to fine tune profiling technologies at all functional levels (viz. transcriptomics, proteomics and metabolomics) in order to address a focused set of questions within a specific conceptual framework, such as functional genomics, integrative and systems biology, translational research or signal transduction and metabolic pathways, for example.
Topics covered by the session are:
- Success stories in biomarker discovery, validation and qualification
- Technological advances in molecular profiling modalities
- Prefractionation methods to increase the depth and throughput of molecular profiling
- Antibody based profiling approaches
- Best storage strategies for biorepositories.
6. Structural and Computational Drug Discovery
Chairs
Alexander Hillisch, Bayer Schering HealthCare AG, DE
Ruben Abagyan, The Scripps Research Institute, US
Computational approaches based on protein structure continue to gain recognition in drug discovery and optimization. In a modern drug discovery environment these approaches are not only applied in lead finding but also target selection, assay development and lead optimization. The impact of protein structure information throughout the entire drug discovery process will be presented in our "Structural and Computational Drug Discovery" topic. The large scale generation of protein structures and the utilization of structural aspects for target selection and HTS assay development will be one focus. You will hear case studies on lead identification through virtual screening and the protein structure guided optimization of compounds. In addition, the recently solved structure of the first pharmacologically relevant GPCR and its implications for structure-based design will be presented.
