Blood-Brain Barrier: Bridging Options for Drug Discovery and Development

By Allan B. Haberman, PhD

TABLES

Table 1.1. CNS Conditions Not Treatable With Current Drugs
Table 3.1. “Rule of Five” for Oral Drugs vs. Rules for CNS-Penetrant Drugs
Table 3.2. Substances Subject to P-gp Efflux from the Brain
Table 4.1. Selected Receptor-Mediated Transport Systems Used for Development of Large-Molecule Drugs That Can Cross the BBB
Table 4.2. ArmaGen’s Pipeline of Large-Molecule Drugs Based on Molecular Trojan Horse (MTH) Technology

FIGURES

Figure 2.1. Structure of Brain Endothelium
Figure 3.1. Role of SLC and ABC Transporters in Active Efflux of Drugs across the BBB
Figure 3.2. Structures of L-DOPA and Dopamine
Figure 3.3. Co-Culture In Vitro Model of the BBB
Figure 5.1. Respondents by Organization Type
Figure 5.2. Increased Involvement by Therapeutic Area
Figure 5.3. CNS Drugs in Early Pipeline
Figure 5.4. Pipeline Indications
Figure 5.5. CNS Drug Development Bottlenecks
Figure 5.6. Increased Involvement by Drug Type
Figure 5.7. BBB R&D Programs
Figure 5.8. BBB Programs: Small Molecule
Figure 5.9. BBB Technology Development
Figure 5.10. BBB Programs: Large Molecule
Figure 5.11. Use of Imaging Methods
Figure 5.12. Types of Imaging Methods

APPENDIX FIGURES

Figure 1A. Respondents by Organization Type
Figure 2A. Respondents by Functional Role
Figure 3A. Respondents by Job Title
Figure 4A. CNS Product Areas Pursued
Figure 5A. Change in CNS Drug Involvement
Figure 6A. Increased Involvement by Drug Type
Figure 7A. Increased Involvement by Therapeutic Area
Figure 8A. Estimated CNS Drug Launches, 2008/2009
Figure 9A. CNS Drugs in Early Pipeline
Figure 10A. Pipeline Indications
Figure 11A. CNS Drug Development Bottlenecks
Figure 12A. BBB R&D Programs
Figure 13A. BBB Programs: Small Molecule
Figure 14A. BBB Programs: Large Molecule
Figure 15A. BBB Technology Development
Figure 16A. Use of Imaging Methods
Figure 17A. Types of Imaging Methods