Antibacterial drug development conference

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7:00 am Registration and Morning Coffee

8:00 Chairperson's Opening Remarks

Thomas D. Gootz, Ph.D., Thomas Gootz Consulting




Overcoming the Difficulties in Antibacterial Drug Development

John Domagala, Ph.D., Senior Director, Research, International Discovery Sourcing Consultants, LLC

The presentation will outline many of the key issues faced in antibacterial drug design and development from markets to bench research. The discussion will highlight discovery approaches using HTS, virtual screening, and natural products, the need for analyzing ADME properties and employing PK/PD studies and will examine historical attrition. From the analysis, approaches to maximize success will be suggested.



8:50 Defining the Medical Need for New Anti-MRSA Antibiotics

Thomas D. Gootz, Ph.D., Thomas Gootz Consulting

9:20 A Novel Oxazolidinone with Enhanced Efficacy Due to Intracellular Accumulation

Andrea Marra, Ph.D., Associate Director, Preclinical Development, Rib-X Pharmaceuticals, Inc.

This presentation will focus on radezolid, an oxazolidinone that was discovered using a structure-based drug design approach. The properties of this drug will be highlighted, in particular its ability to accumulate inside cells, and how they impact efficacy in preclinical infection models.

9:50 Networking Coffee Break

10:15 New Oxazolidinone Antibacterial Agents - What Have we Learned?

Paul Aristoff, Ph.D., President and Founder, Aristoff Consulting, LLC

10:45 Structurally Novel Tetracyclines with MRSA Activity

Roger B. Clark, Ph.D., Director of Medicinal Chemistry, Tetraphase Pharmaceuticals, Inc.

11:15 Delafloxacin: A Broad Spectrum Quinolone with Coverage Against MRSA

Eric Burak, Ph.D., Vice President, Preclinical and Early Clinical Development, Rib-X Pharmaceuticals, Inc.

The distinguishing properties of delafloxacin will be discussed, including its in vitro potency, efficacy in preclinical models of infection, and how it will fit in the clinic.

12:00 pm Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own

1:00 Break


1:25 Chairperson's Remarks

Klaus Dembowsky, M.D., Ph.D., Head, Protein Epitope Mimetics; Medical Director, Polyphor Ltd.

1:30 Directed Expression and Characterization of Drug Resistance Determinants

Herbert Schweizer, Ph.D., Professor, Microbiology, Immunology and Pathology, Colorado State University

Bacterial genomes encode a multitude of putative drug resistance mechanisms. The paucity of drug resistant clinical isolates for many bacterial species hampers characterization and evaluation of clinical importance of these suspected resistance determinants. We developed broad-host-range genetic methods for directed expression and characterization of drug resistance determinants in Gram-negative bacteria.

2:00 Stable Isotope Enhanced Antibiotics

Graham Timmins, Ph.D., Associate Professor, Medicinal Chemistry,College of Pharmacy, University of New Mexico

Stable isotope effects are being used to optimize PK/PD of drugs, generating NCEs with very little risk of failure. We show how novel isotope effects can be used to provide increased antimicrobial action, using a TB as an example, in which we have increased efficacy in a mouse model by ~ 5 fold.

Gram - Negative Infections

2:30 Ribosome Antibiotic Binding (TM): Defining New Frontiers for the Design of Novel Antibiotics for MDR Gram-Negative Infections

Zoltan Kanyo, Ph.D., Scientist, Structure-Based Drug Design, Rib-X Pharmaceuticals, Inc.

This talk will highlight how our RAB platform -- through the solution of hundreds of crystal structures of known and new antibiotics -- has defined a featureful space for the design of new antibiotics that work by inhibiting the large ribosomal subunit. Additionally, it will discuss the molecular property subspace that is key to accessing Gram-negative membranes. Taken together, these have allowed us to design three completely new antibiotic lead series that have been tuned for Gram-negative activity and efficacy in animal models of infection.

3:00 Selected Oral Poster Presentation

3:15 Networking Refreshment Break, Poster and Exhibit Viewing

4:00 Structure-Guided Discovery of (S)-3-(aminomethyl)benzo[c][1,2]oxaborol-1(3H)-ol hydrochloride (ABX): A First in Class Antibacterial for Gram-Negative Infections

Vincent Hernandez, Senior Scientist, Medicinal Chemistry, Anacor Pharmaceuticals

New classes of antibacterial agents are needed to circumvent pre-existing resistance mechanisms. As an extension of our work on fungal leucyl-tRNA synthetase (LeuRS) inhibitors, we have used Co-crystal structures of Escherichia coli LeuRS-tRNA to rationally design compounds with antibacterial activity that inhibit LeuRS by the novel oxaborole tRNA trapping (OBORT) mechanism. This has led to the discovery of ABX, the first member of a new class of 3-aminomethyl benzoxaborole antibiotics with potent activity against Gram-negative bacteria.

4:30 POL7080 and a Novel Class of Antibiotics for Treatment of Gram-Negative Infections Based on Protein Epitope Mimetics Technology

Klaus Dembowsky, M.D., Ph.D., Head, Protein Epitope Mimetics; Medical Director, Polyphor Ltd.

Using the Protein Epitope Mimetics (PEM) Technology a novel class of antibiotics has been identified by Polyphor for treatment of Gram-negative infections. POL7080 is highly potent, selective and efficacious against Pseudomonas aeruginosa and has completed preclinical development. POL7080 and related PEM molecules act via a novel mechanism on membrane proteins of Gram-negative bacteria and may thus provide novel treatment regimes for these infections. The mode of action and properties of POL7080 will be described.

5:00 New Agents for Multidrug-Resistant Gram-Negative Bacteria

Malcolm Page, Professor; Head of Biology, Research, Basilea Pharmaceutica International

The pipeline for agents covering multidrug-resistant Gram-negative bacteria, especially P. aeruginosa and Acinetobacter spp. will be briefly reviewed. Basilea’s candidate, BAL30072, will be used as a case study for development of specific narrow-spectrum agents for these troublesome pathogens.

5:30 Networking Cocktail Reception in the Exhibit Hall

6:30 End of Day

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