Goals and Objectives:
The discovery and development of quality drug leads and clinical candidates, that will eventually become novel drugs, remains a significant challenge to pharmaceutical scientists. It is increasingly clear that integration of drug-like properties into the early stages of drug discovery is advantageous to efficient and effective drug development. Critical issues of compound selection and quality, safety, pharmacokinetics and formulation will be addressed. Symposia and speakers have been selected to enhance our collective knowledge on the discovery and development of novel lead molecules that have drug-like properties and can successfully lead to clinical development candidates. Key areas of focus will include state-of-the-art techniques to mine SAR, identify promising lead compounds, study drug-like properties of leads as they progress through optimization, screen for early safety concerns, and novel approaches to early formulation. The discussions will be targeted toward academic and industrial scientists from the disciplines of medicinal chemistry, biology, pharmacology, DMPK, toxicology, and formulation.
This conference on Drug Discovery Strategies will provide a forum for pharmaceutical scientists to exchange ideas on the state-of-the-art techniques to study drug discovery, enhance knowledge about the relative importance of drug-like properties, and provide an opportunity to learn of the cutting edge science in this area through seminars by invited speakers.
Workshop Agenda
Sunday, May 18
5:00 pm - 7:00 pm Main Lobby
Registration
Monday, May 19
7:00 am - 5:30 pm Main Lobby
Registration
8:00 am Salons F-J
Welcome and Opening Remarks
Jeffrey Silverman, Ph.D.
Sunesis Pharmaceuticals, Inc.
Michael J. Hageman, Ph.D.
Bristol-Myers Squibb Company
8:30 am
Keynote Address:
Innovative Preclinical Strategies to Increasing Productivity in Drug R&D: Finding Medicines
Michael Silber, Ph.D., Pharm. D.
University of California, San Francisco
9:30 am - 12:00 pm Salons F-J
TRACK A - CRITICAL ISSUES FOR CANDIDATE SELECTION—API SYNTHESIS AND CHARACTERIZATION
Moderator
E.F. “Gene” Fiese, Ph.D.
Pharmaceutics Consultant
9:30 am
Candidate Nomination to GMP API Supplies: Issues and Challenges
Thomas C. Crawford, Ph.D.
Tempo Pharmaceuticals, Inc.
10:10 am
Physical-chemical Characterization of API
E.F. “Gene” Fiese, Ph.D.
Pharmaceutics Consultant
10:50 am
Exploratory Development Strategies and Tactics in the Selection of Drug Form
George J. Quallich, Ph.D.
Pfizer Inc.
11:30 am
Panel Discussion
9:30 am - 12:00 pm Baden Room
TRACK B – TOOLS FOR DRUG DISCOVERY—ASSISTING LEAD SELECTION SCREENING AND SAR
Moderator
Michael J. Hageman, Ph.D.
Bristol-Myers Squibb Company
9:30 am
A Specific Mechanism for Non-specific Inhibition
Brian Shoichet, Ph.D.
University of California, San Francisco
10:10 am
Leveraging ADME Screens to Choose Better Leads
Debra Luffer-Atlas, Ph.D.
Eli Lilly and Company
10:50 am
Mining SAR with a Functional Group Approach
Steve Johnson, Ph.D.
Bristol-Myers Squibb Company
11:30 am
Panel Discussion
12:00 pm - 1:00 pm Salons A-E
Lunch with Exhibits
Complimentary to all attendees
1:30 pm - 4:40 pm Salons F-J
TRACK A - CRITICAL ISSUES FOR CANDIDATE SELECTION—FORMULATION DESIGN STRATEGIES
Moderator
Michael J. Hageman, Ph.D.
Bristol-Myers Squibb Company
1:30 pm
Assessment and Characterization of Colloids in the Discovery Setting
Roy J. Haskell, Ph.D.
Bristol-Myers Squibb Company
2:10 pm
Role of Supersaturation in Enhancing Biological Exposure in Preclinical Models
Ping Gao, Ph.D.
Abbott Laboratories
2:50 pm
Formulation Strategies for Animal DMPK, Pharmacology and Toxicology Evaluation
James Wesley, Ph.D.
Eli Lilly and Company
3:30 pm
Linking of Physical-chemical Characteristics with Formulation Strategies and “First in Human” Formulations
Gregory E. Amidon, Ph.D.
University of Michigan
4:10 pm
Panel Discussion
1:30 pm - 4:40 pm Baden Room
TRACK B – TOOLS FOR DRUG DISCOVERY/TOOLS FOR GUIDING LEAD OPTIMIZATION OF DMPK
Moderator
Michael Silber, Ph.D., Pharm. D.
University of California, San Francisco
1:30 pm
Small Molecule Discovery in the Modern World
Michael D. Varney, Ph.D.
Genentech, Inc.
2:10 pm
Optimizing CYP Inhibition Assays for Assessing Drug-drug Interaction Potential in Drug Discovery and Lead Optimization
Larry Wienkers, Ph.D.
Amgen, Inc.
2:50 pm
Approaches to Minimize the Bioactivation Potential of 11-Beta HSD Inhibitors in Lead Optimization
Deepak Dalvie, Ph.D.
Pfizer Inc.
3:30 pm
Trials and Tribulation in the Discovery of a Cathepsin K Inhibitor
Deborah A. Nicoll-Griffith, Ph.D.
Merck and Company
4:10 pm
Panel Discussion
5:00 pm - 6:30 pm Salons A-E
Reception with Exhibits
Tuesday, May 20
7:00 - 5:00 pm
Registration
8:00 am - 11:10 am Salons F-J
TRACK A - CRITICAL ISSUES FOR CANDIDATE SELECTION—CHARACTERIZATION OF ADME PROPERTIES
Moderator
Jeffrey Silverman, Ph.D.
Sunesis Pharmaceuticals, Inc.
8:00 am
Characterization of Metabolites: Implications for Drug Discovery and Development
Gary L. Skiles, Ph.D.
Amgen Inc.
8:40 am
Implications of Efflux Transporters during Lead Optimization
Thomas J. Raub, Ph.D.
Eli Lilly and Company
9:20 am
Adding Value to the Discovery Process through the Application of Pharmacokinetic/Pharmacodynamic Principles
George Tonn, Ph.D.
Amgen Inc.
10:00 am
Whole-body, Micro-autoradiography, MALDI-MS, NanoSIMS, Cryo-Imaging, and PET: Integrated Approaches for Studying Tissue Distribution, Metabolism, and Transport of Biologicals across Tissue Compartments
Alfred Lordi, M.S.
QPS Pharmaceutical Services
10:40 am
Panel Discussion
8:00 am - 11:30 am Baden Room
TRACK B - TOOLS FOR DRUG DISCOVERY—ADVANCES IN ANALYTICAL TECHNOLOGIES
Moderator
Tim Carlson, Ph.D.
Amgen Inc.
8:00 am
Application of LTQ-Orbitrap Mass Spectrometry for Metabolite Identification
Ji Ma, Ph.D.
Amgen Inc.
8:40 am
Novel LC/MS Approaches for Higher Throughput Screening of Reactive Metabolites in Lead Optimization
Mingshe Zhu, Ph.D.
Bristol-Myers Squibb Company
9:20 am
Accelerator MS and Microdosing for Human Metabolism, PK, and Target Confirmation
John S. Vogel, Ph.D.
Vitalea Science
10:00 am
Impact of Affinity Mass Spectrometry on Antibodydrug Conjugate Development
Keyang Xu, Ph.D.
Genentech, Inc.
10:40 am
Panel Discussion
11:30 am - 1:00 pm Salons A-E
Lunch with Exhibits
1:00 pm - 4:20 pm Salons F-J
TRACK A - CRITICAL ISSUES FOR CANDIDATE SELECTION—CHARACTERIZATION OF TOXICOLOGY PROPERTIES IN CANDIDATES
Moderator
Bruce D. Car, Ph.D.
Bristol-Myers Squibb Company
1:00 pm
Addressing Metabolite Related Toxicology Concerns in Early Development
William G. Humphreys, Ph.D.
Bristol-Myers Squibb Company
1:40 pm
Safety and Cardiovascular Toxicology
Derek Leishman, Ph.D.
Eli Lilly and Company
2:20 pm
Mechanistic and Target Based Toxicology
Kyle L. Kolaja, Ph.D.
Roche
3:10 pm
Strategies, Logistics and Organizational Impact for Improved Toxicological Properties
Bruce D. Car, Ph.D.
Bristol-Myers Squibb Company
3:50 pm
Panel Discussion
1:00 pm - 4:20 pm Baden Room
TRACK B - TOOLS FOR DRUG DISCOVERY—ADVANCES WITH IN SILICO METHODS
Moderator
Stefan Steyn, Ph.D.
Pfizer Inc.
1:00 pm
In Silico Drug Design Strategies
Stefan Steyn, Ph.D.
Pfizer Inc.
1:40 pm
Integration of In Silico Models in Drug Design
Hua Gao, Ph.D.
Pfizer Inc.
2:20 pm
Computational Toxicology: New Methods and Models
Sean Ekins, D.Sc., Ph.D.
Arnold Consultancy and Technology
3:10 pm
Turning Uncertain, Multivariate Data into Effective Decisions
Matthew Segall, Ph.D.
BioFocus DPI
3:50 pm
Panel Discussion
Wednesday, May 21
7:00 - 12:00 pm Main Lobby
Registration
8:00 am - 12:00 pm Salons F-J
Preclinical Data to Predict Developability
Moderator
Lan Xiao, Ph.D.
Bristol-Myers Squibb Company
8:00 am
Predicting the Human Dosage Regimen from Preclinical Data—How Confident are We?
Mario Monshouwer, Ph.D.
Roche
8:50 am
Predicting Human Toxicity from Preclinical Tools—Reality or Myth?
Donna Dambach, VMD, Ph.D.
Genentech, Inc.
9:40 am
Predicting Human Metabolism—Are We There Yet?
Debra Luffer-Atlas, Ph.D.
Eli Lilly and Company
10:30 am
Specialized Formulations Enhancing Oral Exposure During Lead Optimization—Converse to Formulation Developability?
Michael J. Hageman, Ph.D.
Bristol-Myers Squibb Company
11:20 am
Invoking Prodrugs as Part of the Lead Optimization Strategy—Should We?
Reza Oliyai, Ph.D.
Gilead Sciences, Inc.
11:50 am
Closing Remarks
Jeffrey Silverman, Ph.D.
Sunesis Pharmaceuticals, Inc.
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