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2008年5月12〜14日 フィラデルフィアにて開催!
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リード最適化を目指す新たな試み

第5回 リード最適化を目指す新たな試み

新たな試みから最適な化合物へ : カタログダウンロード(英語版PDF)

5月13日(火)〜14日(水)

薬物代謝の分析と反応性代謝物のプロファイリングにおける分析戦略

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

薬物相互作用 – CYP阻害のスクリーニング

Utilizing New Technologies for CYP Inhibition Screening at Bristol-Myers Squibb
Tatyana Zvyaga, Ph.D., Senior Research Investigator, Lead Discovery, Bristol-Myers Squibb

薬物輸送体

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.

リード最適化へ向けた計算論アプローチ

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


推奨ショートコース *

5月12日(月)午前 (SC3) 薬物代謝の概説I: 代謝体のプロファイリング

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.

5月12日(月)午後 (SC4)薬物代謝の概説II* 薬物相互作用に関する懸念と現状の取り組み

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.

* こちらのコースへの出席に際しては別途お申し込みが必要となります。
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