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Scientific Advisory Board
Jonathan Mason, Ph.D., Divisional Director, Early Lead Generation and Computational Chemistry, Lundbeck Research DK
Mark Murcko, Ph.D., Vice President and Chief Technology Officer, Vertex Pharmaceuticals Inc.
Tudor I. Oprea, Ph.D., Professor & Chief, Biochemistry & Molecular Biology Biocomputing, University of New Mexico School of Medicine
Thursday, October 11
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SCREENING AGAINST
MULTIPLE TARGETS
(Shared Session with Drug Repositioning Summit) |
12:30 pm Registration
1:30 Chairperson’s Remarks
David M. Manyak, Ph.D., Executive Vice President, Drug Discovery Services, Caliper Discovery Alliances and Services, Caliper Life Sciences, Inc.
Featured Presentation
1:40 Is Repositioning a Viable Option for Creating Differentiated Medicines?
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Rebecca A. Taub,
M.D., Vice President, Metabolic Diseases, F. Hoffmann-La Roche, Inc.
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- How do we create internal buy-in for this concept and how do we establish partnerships with biotech and academia to create a case for investing in repurposed drugs?
- What are the best wet-lab and in silico technologies that can be applied to identify new disease indications for promising drugs?
- Once the data suggests a new way forward, how can we make such assets a high priority in our companies and/or use these to gain access to other types of external innovation?
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| 2:15 Automated Robotic Molecular Profiling in Cells for New Therapeutic Directions
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Jeremy S. Caldwell, Ph.D., Director of Molecular and Cell Biology, Genomics Institute of the Novartis Research Foundation
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Small molecule cross reactivity against multiple targets can simultaneously afford broad therapeutic utility and problematic non-specific effects in man. Quantitative methods to rapidly characterize molecules in a broad array of cellular assays would reveal the range of functions associated with small molecules and impart a more thorough profile of drug candidates early in the drug development process. Here we describe a high-throughput approach to discover the multiple activities of small molecule libraries analyzed in parallel against a broad array of phenotypic cellular assays, and the robotic infrastructure necessary to perform these measurements.
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2:45 Poster Session, Exhibit Viewing and Refreshment Break
| 3:15 An Efficient Platform for Genetic Target and Compound Positioning
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David Grass, Ph.D., Vice President, Scientific Operations, Caliper Discovery Alliances and Services, Caliper Life Sciences, Inc.
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Given the challenges facing the biopharmaceutical industry, including increased drug discovery and development timelines, fewer IND and NDA submissions per R&D dollar investment, and diminishing drug exclusivity timelines, it has become extremely important to identify potential indications for both genetic targets and compounds as early and efficiently as possible. Caliper Discovery Alliances and Services
(CDAS, Xenogen Biosciences) has created a broad platform which uses mice to comprehensively characterize genetic targets and compounds. This platform utilizes
in vivo assays that are relevant to most of the major therapeutic areas. For genetic targets, this platform allows for efficient target validation and early positioning of potential therapeutics. For compounds, this platform identifies unanticipated “pre-positioning” opportunities for earlier stage compounds as well as repositioning opportunities for existing therapeutics and clinical development compounds.
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3:45 Integrative In Vitro Safety Pharmacology Profiling to Predict Clinical Adverse Effects
Laszlo Urban, M.D., Ph.D., Global Head, Safety Profiling, Novartis Institutes for BioMedical Research
In vitro
safety pharmacology is applied during lead selection and lead optimization to predict possible adverse drug reactions. Various panels of
biochemical and functional assays are used in conjunction with the analysis of physicochemical
properties of molecules. Recently developed in silico tools enhanced the predictive value of early safety profiling and made it a valuable part of integrative risk assessment to aid selection of scaffolds and individual compounds for further development.
4:15 Ceftriaxone and Results of Large Scale Screening Efforts
Jill Heemskerk, Ph.D., Extramural Research Program Neuroscience, National Institute of Neurological Disorders and Stroke
The approved drug screening approach will be discussed and examples from this effort will be discussed. This includes Ceftriaxone. An additional success story will be covered based on indoprofen for another neurodegenerative disease (SMA). This program required some chemistry to transform indoprofen into a suitable drug for a CNS indication. We have also developed a shelved compound collection for distribution.
| 4:45 Panel Discussion: How to Choose a Compound with the Best Profile |
5:15 Close of Day
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