トレーニングセミナー | 22nd Annual Discovery on Target 2024 公式サイト

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Cambridge Healthtech Instituteのトレーニングセミナーは、学術的な理論とその背景事情を幅広くカバーすると共に、実際の事例研究や直面した課題、採用された解決策などを提供します。個々のトレーニングセミナーでは正規のレクチャーと対面型の議論・活動を併用して、学習体験を最大化できるようにしています。このトレーニングセミナーは、経験豊富な講師が司会し、現在の研究内容に適用できる内容に焦点を当てると共に、この分野の初心者にも重要なガイダンスを提供します。

トレーニングセミナーは対面形式でのみ開催されます。

2024年10月1日（火） 8:00 am - 6:00 pm | 2024年10月2日（水） 8:00 - 10:00 am

TS8A: GPCR Pharmacodynamics: Kinetics, Allosterism, and Biased Agonism in Pharma Discovery

This training seminar describes models and tools that extend GPCR pharmacology into new therapeutic areas. I review the new data characterizing the allosteric nature of GPCRs and how this can be applied to the discovery of new drugs. Discussion emphasizes characterization of Biased Agonists, Positive Allosteric Modulators (PAMs), and Negative Allosteric Modulators (NAMs) in practical terms for application to drug discovery.

Topics to be Covered:

The Role of Pharmacology in Drug Discovery / Determining Mechanism of Drug Action / Tools of Pharmacology: Dose-Response Curves, Assays / Pharmacologic Principles: Affinity / Efficacy
What is Efficacy? / The Black/Leff Operational Model / Biased Signaling / Selecting GPCRs as Drug Targets / Kinetics as a Major Player in GPCR Drug Selection
Allosteric Protein Function / The 2 Unique Functions of Allosteric Modulators / 'Induced-Bias' and Allosteric Probe Dependence / Quantifying Allosteric Function / NAMs, PAMs, and PAM-Antagonists / Case Studies: 'Know Your Molecule'

INSTRUCTOR BIOGRAPHIES:

Terrence P. Kenakin, PhD, Professor, Pharmacology, University of North Carolina at Chapel Hill

Beginning his career as a synthetic chemist, Terry Kenakin received a PhD in Pharmacology at the University of Alberta in Canada. After a postdoctoral fellowship at University College London, UK, he joined Burroughs-Wellcome as an associate scientist for 7 years. From there, he continued working in drug discovery for 25 years first at Glaxo, Inc., then Glaxo Wellcome, and finally as a Director at GlaxoSmithKline Research and Development laboratories at Research Triangle Park, North Carolina, USA. Dr. Kenakin is now a professor in the Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill. Currently he is engaged in studies aimed at the optimal design of drug activity assays systems, the discovery and testing of allosteric molecules for therapeutic application, and the quantitative modeling of drug effects. In addition, he is Director of the Pharmacology graduate courses at the UNC School of Medicine. He is a member of numerous editorial boards, as well as Editor-in-Chief of the Journal of Receptors and Signal Transduction. He has authored numerous articles and has written 10 books on pharmacology.

2024年10月2日（水） 1:45 - 5:15 pm | 2024年10月3日（木） 8:00 am - 4:35 pm

TS7B: Drug Exposure at the Target: The Role of ADME and Pharmacokinetics

This training seminar describes how pharmacokinetics (PK) affects drug exposure at the intended target. The seminar opens with a foundation of clinical PK including the determination of key PK parameters from Cp-time data. Seminar materials also cover common preclinical ADME assays that allow estimation of a compound's human PK properties. The materials bridge the idea of a compound's PK and its observed pharmacodynamic effects (PD) through coverage of PK/PD modeling. Various drug modalities (e.g., small molecules, antibodies, and peptides) illustrate the concepts of the seminar.

Session 1:

Drug discovery-typical order of operations
ADME and key pharmacokinetic parameters
Modeling Cp-time curves from an IV dose
Modeling Cp-time curves from an oral dose

Session 2:

Oral drug space and membrane permeability
Metabolic stability and intrinsic clearance
Plasma, PPB, and the free drug hypothesis
Compartment modeling and PBPK

Session 3:

Pre-formulation and formulation
Preclinical species and allometric scaling
Non-small molecule drug modalities
PK/PD modeling

INSTRUCTOR BIOGRAPHIES:

Erland Stevens, PhD, James G. Martin Professor, Department of Chemistry, Davidson College

Erland Stevens is formally trained as a synthetic organic chemist, with a PhD from the Department of Chemistry at the University of Michigan at Ann Arbor. He specialized in nitrogen heterocycle synthetic methodology. After completing his postdoctoral research at The Scripps Research Institute in La Jolla, CA, he joined the chemistry faculty at Davidson College in Davidson, NC. In addition to teaching organic chemistry, he created an undergraduate medicinal chemistry course and later published a textbook, Medicinal Chemistry: The Modern Drug Discovery Process, with Pearson Education. He then created an online medicinal chemistry course, which has been continuously revised and publicly available for approximately 10 years. He subsequently worked with Novartis to create additional online materials that are used with employees for continuing education purposes. He maintains an interest in the computational prediction of pharmacokinetic parameters based on structural features of drug-like structures.

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