Main Conference Day 2: Wednesday, January 27, 2010

8:35 Welcome Address And Chairperson’s Opening Remarks

Update on Antifungals

8:45 Approaches To Novel Antifungal Therapies

• Finding antifungal targets
• Understanding the role of resistance mechanisms
• Biologics and other novel approaches
• Evaluating approaches to modify existing antifungals (polyenes and azoles)
• Introducing novel therapies (peptides, oligonucleotides, and monoclonal antibodies (MAbs))

Neil Ryder
PhD, Executive Director, Infectious Diseases
Novartis Institutes for Biomedical Research

9:30 Addressing Serious Fungal Infections & Broad Spectrum Clinical Candidates

• Discussing fungi present in the gastrointestinal tract (Candida) or in the environment (Aspergillus)
• Displaying a novel small molecule fungal Hos2 inhibitor that enhances the activity and spectrum of current azole treatments against fungal pathogens when co-administered with azoles
• Demonstrating how MGCD290 enhances the azole susceptibility of common fungal pathogens such as Candida and Aspergillus species
• Possessing a broad-spectrum inhibitory profile for both class A and class C beta-lactamase enzymes, including extended spectrum betalactamases (ESBLs)
• Overcoming resistance in beta-lactam-resistant organisms such as Pseudomonas aeruginosa

Jeffrey M. Besterman
PhD, Executive Vice President, R & D and CSO
MethylGene Inc.

Gram-Positive & Gram-Negative Bacteria

11:00 Multi-Drug Resistant Gram-Negative Bacteria - Real Challenges And Potential Solutions

• Identifying problem pathogens (drug-resistance in E. coli, K. Pneumoniae, P. aeruginosa and A. baumannii)
• Examining resistance mechanisms in E. coli and K. pneumoniae
• Evaluating resistance mechanisms in P. aeruginosa and A. baumannii
• Activity of new agents, and compounds in late-stage clincal development, against MDR
• Activity of experimental compounds in early stage clinical development

Malcolm Page
PhD, Head, Biology
Basilea Pharmaceutica Ltd.

11:45 Structure-Guided Discovery Of (S)-3-(aminomethyl)benzo[c][1,2]oxaborol-1(3H)- Ol Hydrochloride (ABX): A First In Class Gramnegative Antibacterial

• Examining structure-based design of boron-containing antibacterial agents
• Editing active site of Leucyl tRNA synthetase as a novel drug target
• In vitro activity of ABX against multi-drug resistant Gram negative bacteria
• Discussing oral efficacy of ABX in mouse thigh infection models

Vincent Hernandez
Senior Scientist, Medicinal Chemistry
Anacor Pharmaceuticals

Novel Therapeutic Approaches

1:30 Bacterial Fatty Acid Synthesis As Target For AFN- 1252, A Novel And Selective-Spectrum Antibiotic For The Treatment Of Staphylococcal Infection

• Unique mechanism of action, selective inhibitor of staphylococcal fatty acid biosynthesis
• Highly potent, optimized to inhibit the staphylococcal FabI enzyme
• Preclinical safety and a selective-spectrum of activity predict minimal antibiotic treatment related adverse effects
• Orally effective in multiple mouse infection models (pneumonia, sepsis, thigh and skin abscesses)
• Well tolerated in phase 1 clinical studies

Nachum Kaplan
PhD, Vice President, Microbiology
Affinium Pharmaceuticals

2:15 Target-Based Screening: Discovery Of Novel Inhibitors Of Bacterial NAD+-Dependent DNA Ligase

• Discussing in vitro validation of DNA ligase as a target for high throughput screening
• Optimizing potency of enzyme inhibition to achieve antibacterial activity
• Linking antibacterial activity to inhibition of DNA ligase
• Achieving in vivo validation of DNA ligase via efficacy in infection model

Scott Mills
PhD, Principal Scientist
AstraZeneca

Future Anti-Infective Drug Discovery Techniques & Strategies

3:30 Anti-Infective Drug Discovery Through Outsourcing And Collaborations

• Examining the current paradigm of anti-infective drug discovery
• Discussing how and why companies are moving compounds ahead when many larger groups have downsized their infectious disease efforts
• Utilizing partners to help overcome significant challenges to public healthcare arising from drug resistant bacteria
• Progression of anti-infective drug discovery and development through the provision of a comprehensive range of highly specialized services to the pharmaceutical, biotechnology and consumer healthcare sectors
• The use and role of the academic collaborator, scientific incubator, CRO and CMO – what they need to know to accelerate drug development
• Current research collaborations for new drug discovery: Big Pharma and Biotech

William Weiss
PhD, Director of Pre-Clinical Services
University of North Texas Health Science Center

4:15 Addressing The Challenge Of Fungal Infections: What Are Our Options?

• Discussing fungi such as Aspergillus fumigatus cause a variety of serious nosocomial infections in immunocompromised patients
• Resulting with their resistance to antibiotics has profound clinical implications
• Displaying the three antibiotic classes which are currently in clinical use for fungal infections: amphotericin, echinocandins and azoles
• Examining why all of these classes have efficacy and toxicity drawbacks
• Identifying and discussing approaches towards achieving this include:
  • Derivatization of echinocandins and azoles
  • Potentiation by modulating resistance mechanisms targeting other fungal functions
  • Importing insights from antiprotozoal and anticancer agents.

Nafsika Georgopapadakou
PhD, Vice President, Research
NovaBay Pharmaceuticals

5:00 End Of Conference & Chairperson’s Closing Remarks

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