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.
TUESDAY, SEPTEMBER 17: 8:00 AM - 7:10 PM –
WEDNESDAY, SEPTEMBER 18: 8:00 AM - 2:45 PM
TS1: Targeting GPCRs for Drug Discovery
This 1.5-day training seminar is designed for medicinal chemists, discovery biologists and all scientists concentrating on discovering and developing drugs against G Protein-Coupled Receptors
(GPCRs). The challenge the seminar addresses is how to predict therapeutic activity – because drug candidate profiles seen in in vitro test systems often do not adequately reflect in vivo responses due to the drug candidate’s
interaction with variable ambient physiology. More specifically, this seminar describes the pharmacological procedures needed to convert ‘descriptive data’ (what we see) to ‘predictive data’ (what will be seen) through
universal pharmacological scales such as affinity, efficacy, cooperativity parameters, offset rates, etc. The desired outcome is to more fully define ligand properties to reduce attrition in late-stage drug development. Three major classes of
GPCR ligands will be discussed: (1) agonists (with special reference to biased signaling), (2) antagonists (with inverse agonists) and (3) allosteric modulators (characterization of NAMs, PAMs). I will illustrate how concepts introduced over the
past 15 years have considerably expanded and revitalized the possibilities for GPCRs as therapeutic targets.
Instructor: Terry Kenakin, PhD, Professor, Department of Pharmacology, University of North Carolina School of Medicine
TS2: An In-Depth Introduction to Drug Metabolism and Applications to Discovery and Development - Detailed Agenda
This 1.5-day lecture-based interactive seminar, which focuses on small molecule drug metabolism, will begin with a historical background
to the origin of the field before reviewing the both well-recognized and more recently discovered drug metabolism pathways. In vitro assays used to access metabolic clearance and medicinal chemistry strategies for modifying structures
to overcome metabolism-dependent clearance during lead-optimization will be discussed. The topic of drug toxicity will be discussed in the context of drugs that are toxic through bioactivation to reactive metabolites, examples of drug structure-toxicity
relationships and the relevance of idiosyncratic toxicity to the pharmaceutical industry. The role of metabolite identification studies in preclinical and clinical development will be compared and the steps involved in identifying and characterizing
metabolites by mass spectrometry will be explained. Advances in the use of in silico tools in the context of drug metabolism will be explored. An overview of the pharmacological properties and functions of drug transporters
and some preclinical approaches to investigate drug transport mechanisms will be presented as well as current regulatory guidance on transporters. This seminar is intended for scientists in either academia or industry who would like to become
more familiar with small molecule drug metabolism.
Instructor: John C.L. Erve, PhD, DABT, President, Jerve Scientific Consulting, Inc.
WEDNESDAY, SEPTEMBER 18: 12:20 - 6:30 PM –
THURSDAY, SEPTEMBER 19: 7:30 AM - 4:10 PM
TS3: Introduction to Small Molecule Drug Discovery and Development - Detailed Agenda
This 1.5-day lecture-based interactive seminar focuses on strategies for identifying drug discovery targets, discovering and characterizing small molecule hits, and
developing structure-activity relationships to advance hits through lead optimization, preclinical development, and clinical evaluation. Participants will learn the stages and processes required to advance programs from idea to clinic, through
examples and case studies. This seminar is intended for scientists in either academia or industry who would like to become more familiar with small molecule drug discovery and development.
Instructor: H. James Harwood Jr., PhD, Founder and CEO, Delphi BioMedical Consultants, LLC
TS4: Practical Phenotypic Screening - Detailed Agenda
Phenotypic drug discovery is experiencing a renaissance in the pharmaceutical industry, based on its successful track record in delivering first-in-class medicines. This approach
offers the promise of delivering both novel targets and chemical matter modulating a disease phenotype of interest. Although phenotypic screening may appear at first sight to be similar to target-based screening, there are some significant differences
between the two approaches. These need to be properly considered and addressed to ensure the greatest likelihood of success for phenotypic drug discovery programs. This seminar will cover a range of relevant topics with a goal of providing practical
information to help prosecute such programs more effectively.
Instructor: Fabien Vincent, PhD, Associate Research Fellow, Discovery Sciences, Pfizer, Inc.
What is a Training Seminar?
Each CHI Training Seminar offers 1.5 days of instruction with start and stop times for each day shown above and on the Event-at-a-Glance published in the onsite Program & Event Guide. Training Seminars will include morning and afternoon refreshment
breaks, as applicable, and lunch will be provided to all registered attendees on the full day of the class.
Each person registered specifically for the Training Seminar will be provided with a hard copy handbook for the seminar in which they are registered. A limited number of additional handbooks will be available for other delegates who wish to attend
the seminar, but after these have been distributed, no additional books will be available.
Though CHI encourages track hopping between conference programs, we ask that Training Seminars not be disturbed once they have begun. In the interest of maintaining the highest quality learning environment for Training Seminar attendees, and because
seminars are conducted differently than conference programming, we ask that attendees commit to attending the entire program, and not engage in track hopping, as to not disturb the hands-on style instruction being offered to the other participants.