ACS ProSpectives Conferences on the Discovery, Development & Production of Pharmaceuticals and Therapeutics

Topics and Tactics in Current Drug Design

Oct 19 – 21, 2008 | Cambridge, MA |The Boston Marriott Cambridge

Overview

The “Topics and Tactics in Current Drug Design” conference was chaired by Dr. Nicholas A. Meanwell, Executive Director of Discovery Chemistry at Bristol-Myers Squibb Research and Development, and Dr. Milind S. Deshpande, Executive Vice President of Research & Chief Scientific Officer of Achillion Pharmaceuticals, Inc.

The expeditious and successful development of drug candidates requires a detailed understanding of drug-target interactions and an appreciation for the many off-target sources of drug failure. This ACS Prospectives conference looked broadly at contemporary topics in drug design and discovery by exploring many of the problems commonly faced by medicinal chemists. Each session emphasized fundamental aspects of drug design, providing comprehensive synopses of the kinds of tactics and strategies that have led to the optimization of drug-target interactions against the backdrop of enhancing drug safety and compound delivery in vivo.

Topics and Speakers:

Plenary Presentation: Norbert Bischofberger of Gilead

Basic Aspects of Drug Design

Patrick Lam, Director, BMS on Molecular Recognition in Drug Design

• Molecular recognition in drug design – novel interactions

Jim McCarthy, Distinguished Research Fellow at Eli Lilly

• Fluorine in Drug Design

Gavin Whitlock of Pfizer UK

• Strategies for Designing Promiscuous Drugs

Martin Stahl, Section Head of Medicinal Chemistry, Roche Basel

• The Importance of Conformation Preferences in Drug Design

Metabolism and Drug Design

F. Peter Guengerich, Harry Pearson Broquist Professor of Biochemistry and Director, Center in Molecular Toxicology, Vanderbilt University

• Oxidizing Enzymes – P450 Structure and Function

Tom Baillie, Vice President, Drug Metabolism & Pharmacokinetics, Merck

• Metabolic Activation and Drug Design – Mechanistic Considerations

Sources of Drug Failure

George Trainor , Executive Director, BMS

• Protein Binding in Drug Discovery

Amit Kalgutkar, Research Fellow, Pfizer

• Tactics for Interfering with Drug Metabolism

Zoran Rankovic, Assistant Director, Medicinal Chemistry, Organon UK

• Medicinal Chemistry Strategies and Tactics for hERG Optimizations

Drug Properties & Drug Delivery

Patrick Stahly of ChemFocus on Tactical Approaches to Designing Drugs with Improved Solubility

• Approaches to Designing Drugs with Improved Solubility

Val Stella, Distinguished Professor of Pharmaceutical Chemistry at the University of Kansas

• A Case for Prodrugs

Matthew Peterson of TransForm Pharmaceuticals on Co-crystals as an Emerging Technique for Drug Formulation

The full-day short course featured Patrick Stahly of ChemFocus teaching on drug formulation and conference organizer Nick Meanwell of BMS and Amit Kalgutkar of Pfizer instructing on toxicophores.