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 - Detailed Agenda
This training seminar is designed for medicinal chemists, biologists and 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 candidates’ 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 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.
Instructors: John C.L. Erve, PhD, DABT, President, Jerve Scientific Consulting, Inc.
Raman Sharma, PhD, Senior Scientist, Biotransformation Group, Medicine Design Department, Pfizer Inc.
Guangqing Xiao, PhD, Director, DMPK, Sunovion Pharmaceuticals 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 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 training seminar will cover a range of relevant topics with a goal of providing practical information to
help prosecute such programs more effectively from assay design all the way to clinical trials.
Instructor: Fabien Vincent, PhD, Associate Research Fellow, Discovery Sciences, Pfizer, Inc.
*Training Seminar times include Plenary Keynote Program, Interactive Breakout Discussions, and Exhibit Hall Refreshment Breaks.
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.