1. 신기술 접목에 의한 신약개발의 발전전망과 전략 LGCI 생명과학 기술원

2. Confidential LGCI Life Science R&D 새 시대 – Post Genomic Era Genome count ‘The genomes of various species including a nematode, a fruit fly,five dozen microbial pathogens, a plant and humans are out, with more to follow.’

3. Confidential LGCI Life Science R&D Genomics Human Genome Sequencing

4. Confidential LGCI Life Science R&D 의약산업과 환경 의약 산업은 년 평균 약 ~11% 정도의 성장을 계속해 왔으며, Genomics 등 생명 과학의 급속한 발전으로 성장세가 더욱 증가할 전망임. Genomics 를 통한 의약 산업 기대 효과  New Drug Target 발굴에 의한 신약 개발 기회 확대  의약품의 부작용 개선 및 안전성 확립  세포 및 조직 재생등 새로운 치료법  질병의 조기 진단 및 예방  유전병, 암, 뇌질환등 불치병 치료  의료 service 의 Portal Information site 활용  보건 의료 산업 전반에 획기적 발전 예상

5. Confidential LGCI Life Science R&D Paradigm shift in drug discovery Predicted Growth Rate of “me-too” Market : Only 7%per year ! Labor intensive Time-consuming Paradigm Shift Genomics HTS Virtual Screening Rational Drug Design “Me too approach” Massive, Random Screening Search New Targets Genomics, HTS, Combichem

6. Confidential LGCI Life Science R&D Paradigm shift in drug discovery Target family approach 60% of the drugs marketed today act upon certain receptors Genomics tells us there are 1,500 such receptors as possible targets It ’ s the same with kinases and proteases(already ~800 kinases have been identified)

7. Confidential LGCI Life Science R&D The Drug Discovery Process Regulatory Approval Phase IB/II Phase IA IND Phase III Assay development Lead optimization Lead generation Target identification and validation Market Hypothesis generation Candidate developmentCommercialization Bottleneck in 1990 Bottleneck in New Millennium

8. Confidential LGCI Life Science R&D Drivers for Speeding Drug Discovery Biotechnology and Genetic Engineering Engineered Cell lines Protein Expression and Production Chemical Libraries Laboratory Automation Micro-plate and Detection Technologies

9. Confidential LGCI Life Science R&D New Methods Chemogenomics Gene-based Focused Chemical Inventory In vitro/Cell-based HTS Bioinformatics Accelerated Drug Discovery Transcriptomics Disease-associated Gene expression profiling Proteomics

10. Confidential LGCI Life Science R&D Cost of Drug Development 136 312 431 635 0 100 200 300 400 500 600 700 Millions $ 1234 1998 Health Economics 1993 Office of Technology Assessments 1991 Tufts University 1979 University of Rochester

11. Confidential LGCI Life Science R&D 3 Key Elements in HTS Software HardwareChemical Library Fast Changing! Fast Improvement!! Most Important factor for High Throughput !!! Increasing ! Most important factor for successful discovery !! Moderately changing! Important when Data becomes larger & larger!! HTS (High Throughput Screening)

12. Confidential LGCI Life Science R&D Needs for HTS Miniaturization –Costs for single testpoint (e.g. reagents) – Disposal (radioactive, biohazard) –Drain of test compounds –Tendency towards assays with limited reagents  Speed –Screening libraries grow steadily – Growing number of assays to be tested  Automation

13. Confidential LGCI Life Science R&D Miniaturization, Why? Total cost to screen 200,000 cpds $100,500 $22,600 $10,940 Reagent Cost Plate Cost 96 Well 384 Well 1536 Well

14. Confidential LGCI Life Science R&D Impact of miniaturization Plate 96 384 1,536 9,600 # of Cpds 88 352 1,408 8,800 # of Plate 2,273 568 142 23 Assay Volume 100  L 20  L 4  L 0.2  L Cost ($) 436,400 87,200 17,400 880 200,000 Compounds

15. Confidential LGCI Life Science R&D Chemical Biology Issue Chemical biology is a process in which the chemist sees the world through a biologist ’ s eyes and vice versa. Genomics provides us with an abundance of new targets, but it is getting increasingly difficult for chemistry to find or synthesize compounds that act on these targets. By combining the expertise of biologists and chemists, we are improving our ability to predict the chemical structures that will optimally bind to a biological target.

16. Confidential LGCI Life Science R&D Chemical Biology Issue Genomics Proteomics The physiology of a disease Experience in pharmacology Rational drug design Targeted scaffolds Libraries of compounds Medicinal chemistry Knowledge networking Biological information Chemical information