2025年トレーニングセミナー（対面のみ）

Cambridge Healthtech Instituteのトレーニングセミナーでは、実際のケーススタディ、遭遇した問題、適用されたソリューションのほか、学術的な理論と背景に関する幅広い説明を提供します。各トレーニングセミナーでは、正式な講義とインタラクティブなディスカッションやアクティビティを組み合わせて、学習体験を最大限に高めることができます。これらのトレーニングセミナーでは、経験豊富な講師が、現在の研究に適用可能な内容に焦点を当て、その分野の初心者に重要なガイダンスを提供します。

Drug Discovery Chemistryによるトレーニングセミナーは、対面のみで提供されます。

2025年4月15日（火）午前 8:00 - 午後 3:35 | 2025年4月16日（水）午前 8:00 - 午後 12:00

TS6A: The Medicinal Chemistry-Pharmacology Interface: The 3 Independent SARs for New Drug Candidates
TS6A: 医薬品化学・薬理学のインターフェース：新薬候補に3つの独立系SAR

This training seminar will cover the three independent structure-activity-relationships (SARs) that must be satisfied for new drug success: (1) Primary Target Activity, (2) Pharmacokinetic Profile, and (3) Safety; with a focus on SAR(1): Primary Target Activity.

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

Seminar Outline:

Day 1 (AM): SAR 1: Primary Target Activity

Affinity: What concentrations are needed in the receptor compartment for target binding?
Efficacy: How do drugs produce cellular response (drugs have many efficacies)? How the combination of signaling effects yields a ‘quality’ of efficacy to cells.

Day 1 (PM): SAR 1: Primary Target Activity (cont.)

Efficacy/how biased-signaling causes complex patterns of efficacy (and how can this be manipulated?).
Allosteric vs. orthosteric interaction of molecules: how allosteric interaction fundamentally differs from orthosteric (same site) interaction.
Kinetics of ligand interaction for in vivo target coverage: the importance of in vivo–restricted diffusion/importance of receptor offset rates for target coverage (PK-PD dissociation)/methods to measure kinetics.

Day 2 (AM): SAR 2—Pharmacokinetic Profile and SAR 3—Safety

SAR 2 (ADME): Methods for modification of candidate ADME properties (modification of ‘druglike’ activity/specific modification of interactions with recognition processes (i.e., hepatic enzymes, transporters).
SAR 3: Safety: Basic safety issues faced early on (cytotoxicity, hepatotoxicity, hERG, Ames test)/translation of in vitro to in vivo activity.

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.

2025年4月16日（水）午後 1:30 - 5:45 | 2025年4月17日（木）午前 10:15 - 午後 5:40

TS6B: Drug Exposure at the Target: The Role of ADME and Pharmacokinetics
TS6B: ターゲットでの薬剤曝露：ADMEと薬物動態の役割

This training seminar describes how pharmacokinetics (PK) affects drug exposure at the intended target. It opens with a foundation of clinical PK including the determination of key PK parameters from Cp-time data. It also covers 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.

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

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 models

Session 3

Preformulation and formulation
Preclinical species and PBPK
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.

*不測の事態により、事前の予告なしにプログラムが変更される場合があります。

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