|
Thursday, October 11
8:00 am Morning Coffee
8:30 Chairperson’s Remarks
Marcel van Duin, Ph.D., Executive Director and Head, Department of Pharmacology, NV Organon
| 8:40 Uncovering Unexploited Biology on Halted Drugs
|
|
Akinori Mochizuki, Ph.D.,
Director, Sosei Co. Ltd. |
|
In order to look for the potential of second biological target on halted drug candidates, Sosei has established a unique business model, the Drug Reprofiling Platform. Our efforts in the last several years are giving some answers to our original questions, is there any possibility to identify a new use on halted drugs, if so, how? Can we develop it for a new indication which was originally un-identified? Our DRP business model and some outcomes will be introduced.
|
| 9:15
Repositioning at Organon - Just for Halted Drugs?
|
 |
Marcel van Duin, Ph.D., Executive
Director and Head, Department of Pharmacology, NV Organon
|
|
Repositioning at Organon started with the
identification of drugs that were discontinued at various stages of the
development process. Based on this compound list, we established a number of
collaborations with repositioning companies. This allowed us to exploit a range
of philosophies and technologies and explore the possibilities in various
therapeutic areas to the fullest. Currently, the concept of exploring the full
therapeutic potential of our compounds, also in earlier phases of discovery, is
catching on. Efforts range from cross-screening sets of compounds on a variety
of targets to a focus search for new indications for compounds.
|
| 9:45 CIPRO: The Creation of a New Blockbuster
|
 |
Hans-Joachim Zeiler, Ph.D., Consultant, Innovation,
Bayer/HighTech Private Equity
|
|
Ciprofloxacin was identified in 1981 as a new, highly attractive antimicrobial agent. The use of knowledge about properties of older drug classes and the creation of a chemical niche allowed Bayer to build in new properties into such a molecule which made it useful for the treatment of severe systemic infections. This drug became one of the biggest successes in the field of antimicrobial therapy.
|
10:15 Poster Session, Exhibit Viewing and Coffee Break
| 10:45 Drug Repositioning Using a Multiplexed
In Vivo Platform: Discovery of MLR-1023, A Repositioned Drug Candidate for Type II Diabetes
|
 |
Michael S. Saporito, Ph.D., Vice President, Research, Melior Discovery Inc.
|
We have developed a unique repositioning approach involving a platform comprised of multiple
in vivo models representing diverse therapeutic areas. The power of this platform is illustrated by our lead compound, MLR-1023. This compound, originally developed for ulcers, exhibits robust activity in a panel of clinically relevant models of type II diabetes and is currently being developed for this indication. Of importance was the identification of a previously unknown molecular target for type II diabetes. This example of Melior Discovery’s approach demonstrates the potential for capturing new indications from existing molecules, and the potential for expanding our understanding of the underlying biological basis of
disease.
|
11:15 Panel Discussion: IP and Practical Issues of Drug Repositioning and Repurposing
Moderator: Kevin Davies, Editor-in-Chief, BioIT World
- Strategies for partnering, gaining patent protection and
freedom to operate
- Cultural and organizational obstacles in repositioning and repurposing
- Best practices and success stories for gaining approval
Additional Panelists
Donald E. Frail, Ph.D.
Thomas Barnes, Ph.D.
Richard B. Smith, Partner, Technology Group, Edwards Angell Palmer & Dodge LLP
12:00 Luncheon Workshop (Sponsorship Available)
or Lunch on Your Own
|
SCREENING AGAINST MULTIPLE TARGETS
(Shared Session with Compound Profiling)
|
1:30 Chairperson’s Remarks
1:40 Featured Presentation
Is Repositioning a Viable Option for Creating Differentiated Medicines? |
|
Rebecca
A. Taub, M.D., Vice President, Metabolic Diseases, F. Hoffmann-La
Roche, Inc. |
- 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?
|
|
| 2:15 Automated Robotic Molecular Profiling in Cells for New Therapeutic Directions
|
 |
Jeremy S. Caldwell, Ph.D., Director of Molecular and Cell Biology, Genomics Institute of the Novartis Research Foundation
|
|
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.
|
2:45 Poster Session, Exhibit Viewing and Refreshment Break
3:15 An Efficient Platform for Genetic Target and Compound Positioning
David Grass, Ph.D, Vice President Scientific Operations, Caliper Discovery Alliances and Services, Caliper Life Sciences
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 as 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.
3:45 Broad-Scale
In Vitro Pharmacology Profiling to Predict Clinical Adverse Effects and for ADME Profiling
Laszlo Urban, Ph.D., Executive Director, Preclinical Profiling Group, Novartis Institute for Biomedical
Research
In vitro safety pharmacology is applied during lead selection and lead optimization to predict possible adverse drug reactions. Various panels of biochemichal and functional asays are used in conjunction with the analysis of physicochemical propertis 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
4:45 A Universal Assay Technology for Re-addressing and Profiling of GPCR Targets with a Non-second Messenger
Approach
Keith R. Olson, Ph.D., Vice President, R&D, DiscoveRx Corporation
DiscoveRx developed a GPCR product portfolio of over 100 targets providing a generic, cell-based assay format suitable for both profiling and HTS applications that monitors GPCR/Arrestin protein interactions. Utility of the assay for addressing new or previously screened targets, and data using this approach for GPCR profiling will be presented.
5:15 Close of Conference
|
