TUESDAY, SEPTEMBER 17 - WEDNESDAY, SEPTEMBER 18
DAY 1: 8:00 AM - 7:10 PM | DAY 2: 8:00 AM - 2:45 PM
TS2: An In-Depth Introduction to Drug Metabolism and Applications to Discovery and Development
DAY 1: TUESDAY
8:00 am - 5:00 pm Seminar Sessions
Lunch also provided.
5:00 pm Seminar Close of Day
5:05 - 6:05 pm Interactive Breakout Discussion Groups
6:05 - 7:10 pm Welcome Reception in the Exhibit Hall with Poster Viewing
DAY 2: WEDNESDAY
8:00 - 11:20 am Seminar Sessions
11:20 am Seminar Concludes
11:20 am - 12:20 pm Lunch on Own
12:20 - 2:00 pm Plenary Keynote Program
2:00 - 2:45 pm Dessert Break in the Exhibit Hall with Poster Viewing
Exhibit Hall Refreshment Breaks also provided.
John C.L. Erve, PhD, DABT, President, Jerve Scientific Consulting, Inc.
About This Training Seminar:
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.
Participants will see the importance of understanding drug metabolism in the different stages and processes required to advance a new chemical entity from discovery through development into the 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 metabolism.
What You Will Learn:
- Historical background to the field of drug metabolism
- Basic drug biotransformation reactions and the enzymes responsible
- Newly recognized drug biotransformation reactions
- In vitro assays used to access metabolism-based clearance
- Medicinal chemistry strategies for overcoming poor metabolic stability
- Bioactivation pathways to reactive drug metabolites
- Role of reactive metabolites in drug toxicity, including idiosyncratic toxicity
- Role of metabolite identification studies in discovery and development
- Four steps for identifying and characterizing drug metabolites by mass spectrometry
- In silico tools to address drug metabolism and reactive metabolite formation
- Pharmacological properties and functions of drug transporters
- Preclinical approaches to investigate drug transport mechanisms
- Role of transporters in drug PK, PD, efficacy, safety, and drug-drug interactions (DDI)
- Impact of transporter studies on drug discovery and development
- Recommendations from the current regulatory guidance and International Transporter Consortium (ITC) whitepapers on transporter evaluation during drug development
C.L. Erve, PhD, DABT, President, Jerve Scientific Consulting, Inc.
John Erve is from Chicago and received degrees in Chemistry (BS, MS) from the University of Chicago and earned a PhD in Toxicology at Oregon State University under the supervision of Dr. Donald Reed. Following postdoctoral work at Vanderbilt (1995-1999)
he joined BD-Biosciences (Woburn, MA) as a Study Director. In 2002, he joined AstraZeneca (Sweden) where he was involved in characterizing reactive metabolites and their protein adducts in an effort to better understand the role of reactive intermediates
in drug toxicity. In 2004 he joined Wyeth (Collegeville, PA) as a Principal Scientist responsible for metabolite identification. Following the merger with Pfizer in 2010, John joined Novartis Institutes of Biomedical Research (Cambridge, MA) as
a Lab Head in Analytical Sciences. John returned to the field of drug metabolism by joining Elan Pharmaceuticals (San Francisco, CA) in 2012 and after Elan was sold, created Jerve Scientific Consulting focusing on helping small biotech companies
in the Bay area with their drug discovery efforts. His research interests include mechanistic toxicology and using mass spectrometry to characterize metabolites and metabolic pathways.
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.