2025年培训研讨会（仅限面对面实体会议）

Cambridge Healthtech Institute的培训研讨会提供涵盖了广泛的学术理论及其背景，以及现实生活中的案例研究和所面临的挑战及适用的解决方案资讯。每个培训研讨会都结合了正式讲座与互动讨论和活动，以让学习成果最大化。以熟练的讲师来主持培训研讨会，以适用于当前研究的内容，并为该领域的初学者提供重要指导。以目前研究的内容为焦点，提供针对在该领域的初学者重要的指南。

Drug Discovery Chemistry的培训研讨会仅限面对面实体会议。

2025年4月15日（星期二）上午 8:00 - 下午 3:35 | 2025年4月16日（星期三）上午 8:00 - 下午 12:00

TS6A: The Medicinal Chemistry-Pharmacology Interface: The 3 Independent SARs for New Drug Candidates

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（星期三）下午 1:30 - 5:45 | 2025年4月17日（星期四）上午 10:15 - 下午 5:40

TS6B: 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. 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.

* 活动内容有可能不事先告知作更动及调整。

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