第5回 先导化合物最佳化之新方法
5月13日(二)～14日(三)
ANALYTICAL STRATEGIES IN STUDYING DRUG METABOLISM AND PROFILING REACTIVE METABOLITES
Addressing Metabolic BioActivation during Lead Optimization
Wei Tang, Ph.D., Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories
Reactive Metabolites and Marketed Drugs: What Is the Evidence and What Are the Consequences?
John C. L. Erve, Ph.D., Principal Research Scientist, Wyeth Research
DRUG-DRUG INTERACTION ― SCREENING FOR CYP INHIBITION
Utilizing New Technologies for CYP Inhibition Screening at Bristol-Myers Squibb
Tatyana Zvyaga, Ph.D., Senior Research Investigator, Lead Discovery, Bristol-Myers Squibb
DRUG TRANSPORTERS
Permeability/Absorption/Transporter Assays in Lead: Role of PAMPA, Caco-2, P-gp and More…
Praveen Balimane, Ph.D., Senior Research Investigator, Metabolism and PK, Bristol-Myers Squibb Co.
COMPUTATIONAL APPROACHES to Lead Optimization
Maximizing Return on Triage Decisions in Early Lead Discovery
Bruce Posner, Ph.D., Senior Principal Scientist, Pfizer Inc.
Side Effect Profile Prediction: How to Avoid "Dirty" Chemical Features in Lead Optimization
Josef Scheiber, Ph.D., Lead Discovery Informatics/Safety Profiling, Novartis Institutes for BioMedical Research
Enhancing Target Design and Selection in the Early Portfolio
Robert Maguire, Ph.D., Senior Principal Scientist, Cardiovascular, Metabolic and Endocrine Diseases, Pfizer Global Research and Development, Groton/New London Labs
RECOMMENDED SHORT COURSE *Separate Registration Required
(SC3) 药物代谢之导论I: 代谢物谱型 (metabolite profiling) (5月12日 9:00am - 12:00pm)
This course will cover novel approaches to performing metabolite identification in drug metabolism, structure toxicity relationships and how useful they are in predicting toxicities of new drugs. This portion of the course will also demonstrate how to improve the decision-making process in structural modification of drug candidates and reduce toxicity and improve metabolic stability and PK.
(SC4) 药物代谢之导论II: 药物相互作用: 考量及现状 (5月12日 2:00pm - 5:00pm)
This portion of the course will cover the role of cytochrome P450 enzymes in drug-drug interactions in addition to illustrating how toxicity screening using biosensors that measure DNA damage can be useful. Strategies to assess the drug interactions and future FDA guidelines will be addressed.
