Lead Generation Strategies and Technologies in Drug Development - Emerging Techniques Such as Antisense Technology Will Allow Innovators to Minimize Costs





Date Published: June 2011

BI Research's report “Lead Generation Strategies and Technologies in Drug Development - Emerging Techniques Such as Antisense Technology Will Allow Innovators to Minimize Costs” provides key data, information and analysis on lead generation and optimization technologies implemented by pharmaceutical companies or contract research organizations. The report provides information on the emerging technologies and the strategies in lead generation along with the need for accelerating the lead generation process. The report also analyses the economic impact of compound attrition at various stages of the lead generation process. It also reviews the outsourcing landscape to the contract research organizations. This report is built using data and information sourced from proprietary databases, primary and secondary research and in house analysis by GBI Research’s team of industry experts.
 

Scope

  • Key technological developments and new approaches including case studies. 
  • Case studies of new technologies and their implementation by companies in drug development industry 
  • Key drivers and restraints that have a significant impact on the market. 
  • Competitive benchmarking of leading CROs, covering their offerings and recent deals in drug development 

Reasons to Buy

  • Compare the key capabilities and models of major technology solution providers with your requirements and optimize your R&D costs 
  • Develop market entry and market expansion strategies by identifying the key drivers and challenges in the global drug development market 
  • Develop effective strategies to maximize the advantages through the understanding of drug development and business models. 

  

 
1.1 List of Tables 7
1.2 List of Figures 7
2 Accelerating Lead Generation: Executive Summary 9
2.1 Decrease in Approval of NME and Increase in R&D Costs are the Major Drivers for Accelerating Lead Generation Process 9
2.2 Using In Silico Technology to Conduct Lead Generation Studies Improves the Quality of Data and Speeds up the R&D Process 10
2.3 Contract Research Organizations are Emerging as Strategic Partners to Improve R&D Efficiency by Reducing Time to Market and Costs 10
3 Introduction 12
3.1 GBI Report Guidance 12
4 The Drug Discovery Process: Defining Lead Generation 14
4.1 Process of Early Preclinical Drug Discovery 14
4.1.1 Pre-discovery 14
4.1.2 Target Identification 15
4.1.3 Target Validation 15
4.1.4 Lead Identification 16
4.1.5 Early Safety Tests 17
4.1.6 Lead Optimization 17
4.1.7 Preclinical Testing 19
4.2 Hit to Lead - Identifying Possible Structure 19
4.2.1 Strategies Used In Generating Potential Lead from Identified Hits 20
4.2.1.1 Hit Evolution 21
4.2.1.2 Isosteric Replacement 22
4.2.1.3 Hit fragmentation 22
4.2.1.4 Fragment Expansion 23
4.3 Role of Lead Generation in the Path of Drug Development 24
5 Lead Generation Strategies in the Pharmaceutical Industry 26
5.1 Massive Decline in Sales - Dependence on Blockbuster Drugs 26
5.2 Need for Accelerating Lead Generation Process 27
5.2.1 Stricter FDA Rules and Regulations for Drug Approval 27
5.2.2 Penetration of Aggressive Generic Companies 28
5.2.3 The Economic Impact of Compound Attrition at Various Stages of Lead Discovery 31
5.2.3.1 Declining Returns on R&D Investment 32
5.2.4 Drought in the R&D Pipeline Products (Low R&D Productivity) 33
5.3 HTS Solutions for ADME Testing 35
5.3.1 In Vitro Studies of Drug Absorption 36
5.3.1.1 Extrapolation of In Vitro Absorption Data 36
5.3.1.2 Extrapolation of Animal Absorption Data 36
5.3.2 In Vitro Studies of Protein Binding 38
5.3.2.1 In Vitro/In Vivo Protein Binding 38
5.3.2.2 Plasma and Tissue Protein Binding 39
5.4 Fragment-Based Drug Discovery 39
5.4.1 Differences between HTS and FBDD 40
5.4.2 Advantages of Fragment-Based Drug Design over High-Throughput Screening 41
5.4.2.1 BACE Case Study: Fragment Approach Delivers Novel Starting Points for Challenging Targets 41
5.4.3 Applications of Mass Spectrometry in Fragment Library Screening 43
5.4.4 Recent Advances in Structure-Based Fragment Docking and Virtual Screening 43
5.4.4.1 Synergies between Structure-Based and Ligand-Based Virtual Screening 44
5.4.4.2 Successes in Virtual Screening 45
5.4.5 Novel Strategy for the Design of A Fluorinated Fragment Library, Named LEF (Local Environment of Fluorine) 45
5.4.5.1 Advances in Label-Free Assay Screening 45
5.4.5.2 Methodologies such as SPR and ITC Save Researchers Time and Money 47
5.4.6 Ligand-Based Approach to In Silico Pharmacology 48
5.5 Antisense Technology as a Strategy 48
5.5.1 Isis Pharmaceuticals 49
5.5.2 CytRx Laboratories 49
5.6 Iterative Focused Screening as a Strategy 49
5.6.1 Merck Frosst Canada 49
6 Emerging Technology in Lead Generation 50
6.1 Improving High Throughput Screening 50
6.1.1 Overview 50
6.1.2 Case Study 50
6.1.2.1 Tessella's PROSPER Optimized GSK's High-Throughput Screening Process 50
6.1.3 Improving In Vitro Assays for HTS 51
6.1.4 Whole Animal Imaging and Microscopy 51
6.1.4.1 Zebrafish as an Ideal Tool for Drug Screening 52
6.2 The Parallel Synthesis Approach 53
6.2.1 In Vitro Methods 53
6.2.2 In Silico Methods - Structure-Toxicity Relationships 53
6.2.2.1 CADD 53
6.3 Computerized Combinatorial Chemistry and 3D Molecular Modeling 54
6.3.1 Overview 54
6.3.1.1 Quantitative Structure Activity Relationship (QSAR) 54
6.3.1.2 Computer Aided Drug Design (CADD) 54
6.3.1.3 Computer Automated Structure Evaluation (CASE) 55
6.3.1.4 Molecular Modeling 55
6.3.2 Service Providers 56
6.3.2.1 IBM Accelrys Collaboration 56
6.3.3 Case Studies 57
6.3.3.1 Accelrys's Discovery Studio Optimized Vaccine Design Process at Novartis Vaccines 57
6.4 Molecular Bioimaging 58
6.4.1 Overview 58
6.4.2 Service Providers 58
6.4.3 Case Study 58
6.4.3.1 Recent Development in Molecular Imaging by Caliper Life Sciences 58
6.5 Omics-Technology and Bioinformatics 59
6.5.1 Overview 59
6.5.2 Service Providers 60
6.5.2.1 CambridgeSoft Developed Diverse Collaborations 60
6.5.2.2 Roche and IBM Partner to Develop Next Generation Gene Sequencing System 61
6.5.3 Case Study 61
6.5.3.1 National Cancer Institute Selected CambridgeSoft to Support Chemical Biology Consortium 61
7 Lead Generation Now and in the Future 63
7.1 R&D Models: Influence on Lead Generation 63
7.1.1 Recent Technology Developments 63
7.2 A Novel Technology to Enhance Fragment-Based Drug Discovery 67
7.2.1 ZoBio's Target Immobilized NMR Spectroscopy Method for Fragment-Based Drug 67
8 Pharmaceutical Outsourcing as a Strategy to Accelerate Lead Generation 70
8.1 Early Stage Drug Development Outsourcing 70
8.1.1 Strategic or Tactical Advantages of Outsourcing 70
8.1.2 Case Study 71
8.1.2.1 Long Term Partnerships with Drug Discovery Service Provider 71
8.2 Emerging Regions in the Global Contract Research Outsourcing Market for Early Stage Drug Development 72
8.2.1 Latin America 73
8.2.1.1 Potential Advantages of Latin American Contract Research Outsourcing Market 73
8.2.2 Central and Eastern Europe (CEE) 74
8.2.2.1 Potential Advantages of Central and East European Contract Research Outsourcing Market 74
8.2.3 India 75
8.2.3.1 Potential Advantages of Indian Contract Research Outsourcing Market 76
8.2.4 China 77
8.2.4.1 Potential Advantages of Chinese Contract Research Outsourcing Market 78
9 Major Contract Research Organizations in Drug Discovery 80
9.1 Cyprotex Discovery Ltd. 80
9.1.1 Business Overview 80
9.1.2 Services 81
9.2 Shanghai ChemPartner 81
9.2.1 Business Overview 82
9.2.2 Services 83
9.3 Covance, Inc. 83
9.3.1 Business Overview 83
9.3.2 Services 84
9.4 Caliper Life Sciences 84
9.4.1 Business Overview 85
9.4.2 Services 86
9.5 GVK BIO 86
9.5.1 Business Overview 86
9.5.2 Services 87
9.6 Jubilant Biosys 87
9.6.1 Business Overview 88
9.6.2 Services 89
9.7 Advinus Therapeutics 89
9.7.1 Business Overview 90
9.7.2 Services 91
9.8 ITR Canada 91
9.8.1 Business Overview 92
9.8.2 Services 92
9.9 MD Biosciences 93
9.9.1 Business Overview 93
9.9.2 Services 94
9.10 PPD, Inc. 94
9.10.1 Business Overview 94
9.10.2 Services 95
9.11 Ricerca Biosciences, LLC 95
9.11.1 Business Overview 95
9.11.2 Services 96
9.12 MPI Research 96
9.12.1 Business Overview 97
9.12.2 Services 97
10 Accelerating Lead Generation - Appendix 98
10.1 Market Definitions 98
10.2 Abbreviations 98
10.3 Research Methodology 99
10.3.1 Coverage 99
10.3.2 Secondary Research 99
10.3.3 Primary Research 100
10.3.4 Expert Panel Validation 100
10.4 Contact Us 101
10.5 Disclaimer 101
10.6 Sources 101