Discovery & Selection of Successful Drug Candidates
May 4 – 7, 2008 | The Mark Hopkins InterContinental | San Francisco, CA
Overview
The 4th annual ACS ProSpectives "Discovery and Selection of Successful Drug Candidates” is again chaired by Dr. Andrew Combs, Executive Director of Incyte, and Dr. Greg Roth, Associate Professor and Director of Medicinal Chemistry and Pharmacology at The Burnham Institute for Medical Research. Together they have gathered another group of highly regarded pharmaceutical industry scientists who will lecture and collectively present about 20 case studies over the course of the two-and-a half-day program.
This conference is geared specifically for medicinal chemists and focuses on the key drivers for discovery of new drug candidates. The program is comprised of four sessions that address the key areas of interest for the practicing medicinal chemist. They are:
- Hits to Leads
- Structure-Based Drug Design
- ADME – Addressing Permeability Issues
- Efficacy vs Toxicity
In each session, four speakers will lecture on their research in a case study format, specifically addressing and providing prospective on the session topic.
On the last day, three VPs of pharmaceutical companies will present “Prospectives from Industrial Leaders –Pharma Yesterday, Today and Tomorrow.” This session will feature presentations on small molecule drugs that have been discovered and advanced through proof of concept, or been successfully marketed by their companies. These leaders will share their perspectives on how the compounds were discovered, lessons learned, and how these lessons have been instituted into their company’s current drug discovery processes.
A full-day short course, “An Introduction to Metabolism,” will be offered Sunday. Organized by Bradley Wong of Amgen, it will feature lectures on metabolism pathways; NMR applications for metabolite ID problems, with case examples; in vitro methods for metabolite profiling/CYP inhibition; and transporter-mediated efflux as an obstacle in discovery of CNS agents.
Speakers
Plenary Speaker
Joshua Boger, President & CEO of Vertex Pharmaceuticals on “Expecting the Unexpected”
Hits to Lead Discovery
Robert Copeland, Vice President of Biology at the Oncology Center of Excellence in Drug Discovery, GlaxoSmithKline, on “Drug-Target Residence Time: An Alternative Approach to Compound Optimization”
Rod Hubbard of Vernalis and Professor at University of York on “Fragments and Drug Discovery”
Dan Sutherlin of Genentech on “CDK2/Cyclin A Inhibitors: Targeting the Cyclin A Recruitment Site with Small Molecules Derived from Peptide Leads”
Samuel Chackalamannil of Schering-Plough on “Discovery of SCH 530348: A Thrombin Receptor (Protease Activated Receptor-1) Antagonist with Potent Antiplatelet Effect”
Structure Based Drug Design
John Mathias of Pfizer on “UK-500001 : Using Structure-Based Design to Identify Novel Inhaled PDE4 Inhibitors for Asthma & COPD”
William Washburn, Metabolic Diseases Chemistry, Research and Development at BMS, on “Discovery of Dapagliflozin, A Potent Selective SGLT2 Inhibitor for Treatment of Diabetes”
Graeme Semple of Arena on “Discovery of Agonists of the Niacin Receptor (GPR109a)”
Scott Sheehan, Head - Discovery Chemistry Research & Technology at Lilly Research Laboratories, Eli Lilly, on “Binding Interactions of Novel Inhibitors of Dipeptidyl Peptidase IV”
ADME – Drug Permeability
Paul Glossop of Pfizer on “Discovery & selection of inhaled long-acting Beta-2 adrenoceptor agonists for asthma & COPD”
Mark Gallop, Senior Vice President of Research at XenoPort on “Harnessing Nutrient Transport Mechanisms to Optimize Drug Absorption and Disposition In Vivo”
Stephen Baker , Director, R&D Program Management at Anacor on “AN2690, A Topical Oxaborole Antifungal For Onychomycosis”
George Hartman of Merck on "Kinesin Spindle Protein (KSP) Inhibitors: Lessons learned from HTS to MK-0731"
Efficacy vs. Toxicity
Vito Sasseville, Veterinary Pathology Fellow in Discovery Toxicology at BMS
Jim Summers, Divisional Vice President of Advanced Technology, Global Pharmaceutical Discovery, Abbott, on “The Impact of Technology on Drug Safety Assessment – Earlier Detection and Understanding of Tox Issues”
Jim Stevens of Eli Lilly
Kay Ahn, Pfizer Global Research and Development, on “The discovery of selective fatty acid amide hydrolase inhibitors for the treatment of inflammatory pain”
ProSpectives from Industry Leaders
Steve Young of Merck on “HIV integrase inhibitors: the chemistry behind the discovery of raltegravir”
William Curatolo presented for Kelvin Cooper, Senior Vice President, Worldwide Pharmaceutical Sciences at Pfizer Global R&D, on “DRUG MOLECULE PROPERTIES: WHETHER TO DESIGN THEM OR FIX THEM”
John Nuss of Exelixis on “Adventures in Kinase Inhibitor Discovery: Application of an Integrated HTS/Combinatorial Chemistry Approach to the Discovery of Novel Inhibitors for Oncology and Metabolic Disease Targets”