2024 ARCHIVES

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TRAINING SEMINARS
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Cambridge Healthtech Institute Training Seminars offer real-life case studies, problems encountered and solutions applied, along with extensive coverage of the academic theory and background. Each Training Seminar offers a mix of formal lecture and interactive discussions and activities to maximize the learning experience. These Training Seminars are led by experienced instructors who will focus on content applicable to your current research and provide important guidance for those new to their fields.


Training Seminars will be offered IN-PERSON ONLY.

Tuesday, October 1, 2024  8:00 am - 6:00 pm | Wednesday, October 2, 2024  8:00 - 10:00 am

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

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

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.

Wednesday, October 2, 2024  1:45 - 5:15 pm | Thursday, October 3, 2024  8:00 am - 4:35 pm

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

Detailed Agenda
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.
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 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.