Cambridge Healthtech Institute的培訓研討會涵蓋了廣泛的學術理論及其背景，以及現實生活中的案例研究和所面臨的挑戰及適用的解決方案資訊。每個培訓研討會都結合了正式講座與互動討論和活動，以讓學習成果最大化。以熟練的講師來主持培訓研討會，以適用於目前研究的內容為焦點，提供針對在該領域的初學者重要的指南。
培訓研討會將僅以面對面型式進行。
2024年10月1日（二） 8:00 am - 6:00 pm | 2024年10月2日（三） 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（三） 1:45 - 5:15 pm | 2024年10月3日（四） 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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