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Home > Healthcare > Pharmaceutical > Drug Discovery
Accelerating Lead Generation: Emerging technologies and strategies
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| Published Date:
June 2009
Published By:
Business Insights
Page Count:
161
Order Code:
R162-950
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- Accelerating Lead Generation: Emerging technologies and strategies
- Executive Summary
- Introduction
- Identifying hits: library design, virtual screening and fragment based drug discovery
- Innovations in biological assay development
- ADME and toxicology in lead generation
- Lead generation strategies in the pharma industry
- R&D models, innovation and future success of lead generation
- Chapter 1 Introduction
- The drug discovery process: defining lead generation
- Hit finding and verification
- Hit optimization
- Lead optimization
- Criteria for potential lead compounds
- Chemistry
- Pharmacology
- Absorption, Metabolism, Excretion, Distribution (ADME) and
- Toxicity
- Chapter 2 Identifying hits: library design, virtual screening and fragment based drug discovery
- Summary
- Introduction
- Hit to lead - identifying possible structures
- Compound selection
- Physiochemical properties
- Chemical optimization and modification of hits
- Engineering novelty
- Beyond HTS - alternative methods for identifying hits
- Fragment-based drug discovery
- Companies involved in FBDD
- Case study: deCODE chemistry & biostructures Inc
- Case study: Zenobia Therapeutics
- Can FBDD generate successful new drugs?
- Technology improvements driving FBDD
- Improving x-ray crystallography
- Improvements in NMR spectroscopy for FBDD
- High concentration biological assays
- Improving biophysical methods
- Improving fragment library design
- Chemistry-based methods
- HTS vs FBDD
- Virtual screening
- Target based virtual screening
- Case study: Epix Pharmaceuticals’
- When to use virtual screening
- Target based virtual screening: challenges
- Ligand based screening
- Commercial virtual screening platforms
- Conclusions
- Chapter 3 Innovations in biological assay development
- Summary
- Introduction
- Improving high throughput screening
- Identifying valid hits
- A quantitative approach to primary screening
- Compound management and quality assessment
- Dispensing
- Informatics and data analysis
- Improving in vitro assays for HTS
- Surface plasmon resonance
- Isothermal titration calorimetry and nanocalorimetry
- Back-Scattering Interferometry
- Differential scanning fluorimetry
- High throughput Mass Spectrometry
- Bio-layer interferometry
- Innovations in cell-based assay technology
- Automated confocal microscopy methods
- Flow cytometry
- Laser scanning cytometry
- Label-free cell-based screens
- Photonic crystal biosensors
- Dynamic mass redistribution
- Impedance-based whole cell biosensors
- Other cell-based assays
- Reverse arrays
- Enzyme Fragment Complementation
- HCS and SAR
- Novel cell types and cultures
- In vivo methods in lead generation
- Zebrafish
- Whole animal imaging and microscopy
- Conclusions
- Chapter 4 ADME and toxicology in lead generation
- Summary
- Introduction
- Assessing ADME characteristics
- Oral absorption
- P-Glycoprotein interactions
- Plasma protein binding
- Clearance
- Metabolic stability
- Selectivity and off-target effects
- Solubility
- Toxicology at the lead generation stage
- In silico structure-toxicity relationships
- Chemoinformatic methods
- Toxicogenomics
- High content screening
- Zebrafish
- Whole animal imaging
- Determining mutagenic and clastogenic potential
- Measuring HERG liability
- Investigating CYP inhibition and induction
- Conclusions
- Chapter 5 Lead generation strategies in the pharma industry
- Summary
- Introduction
- Lead generation teams
- Case studies
- Bayer
- Boehringer Ingelheim
- Millennium Pharmaceuticals (Takeda)
- Conclusions
- Chapter 6 R&D models, innovation & future success of lead generation
- Summary
- Introduction
- R&D models: influence on lead generation
- R&D models
- Outsourcing and offshoring
- Dealing with academia
- Pharma collaboration - ‘Co-opetition’
- Innovation and the future
- Targets and HTS
- Focus on RNA
- Focus on lead optimization
- Nanochemistry - returning chemistry to its central role in drug discovery
- Lead generation now and in the future
- Chapter 7 Appendix
- Primary research methodology
- Acknowledgments
- Glossary
- Index
- Bibliography
- List of Figures
- Figure 1.1: Pharma industry productivity decline (1999-2008)
- Figure 1.2: Patent losses occurring between 2008-2014
- Figure 1.3: The drug discovery process
- Figure 1.4: Example of a lead generation workflow
- Figure 1.5: Technologies involved in lead generation
- Figure 2.6: Use of structural information in structure-based drug design
- Figure 2.7: Examples of the chemical structures of compounds discovered using FBDD
- Figure 2.8: ZoBio’s target immobilized NMR spectroscopy method for fragment-based drug discovery
- Figure 3.9: Areas of innovation in high throughput screening
- Figure 3.10: Acoustic droplet ejection
- Figure 3.11: Attributes required of software for HTS data storage and analysis
- Figure 3.12: Kinetic characterization of 5 lead series using SPR (Biacore)
- Figure 3.13: Bio-Layer Interferometry from ForteBio
- Figure 3.14: Advantages of cell-based screening in HTS
- Figure 3.15: Principle of detection: cell based assays with the Epic system from Corning
- Figure 3.16 Principle of the EFC assay for a biochemical target: HitHunter from DiscoveRx
- Figure 4.17: ADME and toxicology data available in high throughput assays
- Figure 4.18: The Safety Intelligence Program from BioWisdom
- Figure 4.19: Examples of assertions in the Safety Intelligence Program from BioWisdom
- Figure 4.20: A typical toxicogenomics workflow in the pharma industry
- Figure 5.21: Key innovations in lead generation technologies
- Figure 5.22: Key activities of medicinal chemists during lead generation
- Figure 5.23: ADME-Tox traffic light criteria in use at Bayer
- Figure 5.24: Discovery-Assays-By-Stage paradigm of Millennium Pharmaceuticals
- Figure 6.25: The microreactor-based lead discovery system
- List of Tables
- Table 2.1: Fragment-based drug discovery: the pros and cons
- Table 2.2 Techniques used to assess fragment binding for FBDD
- Table 2.3: Examples of companies with product pipelines derived from FBDD
- Table 2.4: Examples of compounds discovered using FBDD
- Table 2.5: Rule of Three criteria for a fragment library
- Table 2.6: Examples of companies offering fragment libraries and collections for FBDD
- Table 2.7: Examples of companies offering software for virtual screening
- Table 3.8: Examples of companies providing software for HTS information storage and analysis 71
- Table 3.9: Emerging technologies for high throughput screening
- Table 3.10: A comparison of free-solution, label-free molecular interaction techniques
- Table 3.11: Examples of recent collaborations between stem cell companies and big pharma for the use of stem cells in drug discovery research
- Table 3.12: Advantages and disadvantages of zebrafish for compound screening
- Table 3.13: Companies offering zebrafish screening products and services
- Table 3.14: Advantages of molecular imaging of whole animals for preclinical studies
- Table 3.15: Half lives of important positron emitting isotopes
- Table 4.16: Examples of contract laboratories offering HCA cytotoxicity screening
- Table 4.17: Examples of higher throughput or miniaturized versions of the Ames test
- Table 6.18: Recent examples of academic drug discovery funding by big pharma
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