Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Keynote Session: Integration of Drug Metabolism Science and Big Data to Inform Precision Medicine
Discussion Leader: Jane Kenny (Genentech, United States)
7:40 pm - 7:55 pm
Opening Remarks
7:55 pm - 8:00 pm
Introduction by Discussion Leader
8:00 pm - 9:00 pm
Sir Munir Pirmohamed (University of Liverpool, United Kingdom)
""The Role of Metabolism Today": Integration of Drug Metabolism Science and Big Data to Inform Precision Medicine"
9:00 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Drug Metabolism by Intestinal Microorganisms
Dr. Ronald Scheline from the University of Oslo delivered a lecture entitled "Drug Metabolism by Intestinal Microorganisms" at the first Drug Metabolism GRC in 1971. The gut microbiome has been a subject of intense interest over the past several years, and it is fitting that this subject should be addressed for the 50th anniversary conference. Presentations in this session will describe recent advances in drug metabolism by the microbiome and the implications for precision therapeutics.
Discussion Leader: Andrew Goodman (Yale University, United States)
9:00 am - 9:30 am
Michael Zimmermann (European Molecular Biology Laboratory, Germany)
"Identifying Gut Microbiome Contributions to Drug Metabolism and Toxicity"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Matthew Redinbo (University of North Carolina at Chapel Hill, United States)
"Molecular Control of Drug Metabolism by the Gut Microbiota"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Nichole Klatt (University of Minnesota, United States)
"Novel Pharmacomicrobiomic Mechanisms Underlying Microbiome-Mediated Influence on Disease"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Peter Turnbaugh (University of California, San Francisco, United States)
"Precision Medicine Goes Microscopic: Zooming in on the Gut Microbiome and Drug Response"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
3:00 pm - 4:00 pm
The GRC Power Hourâ„¢
The GRC Power Hourâ„¢ is designed to address diversity and inclusion in the scientific workplace by providing a safe environment for informal and meaningful conversations amongst colleagues of all career stages. The program supports the professional growth of all members of our communities, including ethnicity, race and/or gender identity by providing an open forum for discussion and mentoring.
Organizers: Klarissa Jackson (University of North Carolina at Chapel Hill, United States) and Francesca Toselli (UCB Biopharma, Belgium)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Drugs of the Future: Probing the ADME Properties of Novel Therapeutics
This session will explore the ADME properties of contemporary therapeutic agents under development (oligonucleotides and proteolysis targeting chimeras), and will discuss strategies for designing peptides for targeted therapeutics.
Discussion Leader: Sara Humphreys (Amgen, United States)
7:30 pm - 7:55 pm
Diane Ramsden (Alnylam Pharmaceuticals, United States)
"DMPK in Microbiome Therapeutic Development"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Laurie Volak (Johnson & Johnson, United States)
"ADME/PK Challenges and Opportunities of Bifunctional Protein Degraders"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Gaurav Bhardwaj (University of Washington, United States)
"Computational Peptide Design for Oral Bioavailability and Blood-Brain Barrier Traversal"
9:15 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Drug Transporters: Advancing Drug Development and Precision Therapeutics
Drug and solute transporters were undiscovered at the time of the first Drug Metabolism GRC. Therefore, novel insights into the mechanisms and functions of membrane transporters will be the focus of this session. Among the topics to be discussed are the role of protein-protein interactions in the function of hepatic and renal transporters prediction of the effect of drug inhibition on the systemic exposure of transporter substrates, structural insights into the interaction of substrates and inhibitors of ABC transporters, and leveraging multidrug efflux transporters to counter bacterial virulence and antibiotic resistance.
Discussion Leader: Kim Brouwer (UNC Eshelman School of Pharmacy, United States)
9:00 am - 9:30 am
Bruno Hagenbuch (University of Kansas Medical Center, United States)
"Protein-Protein Interactions of Hepatic and Renal Drug Uptake Transporters"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Pallabi Mitra (Boehringer Ingelheim, United States)
"Prediction of In Vivo Exposure Changes due to Hepatic Transporter Inhibition - A Possibility or Still Futuristic"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Kaspar Locher (ETH Zurich, Switzerland)
"Structural Insight into Drug and Inhibitor Interactions with Human ABC Transporters"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Gauri Rao (University of North Carolina at Chapel Hill, United States)
"Multidrug Efflux Pump Inhibitors: Effective Strategy to Sabotage Bacterial Virulence and Antibiotic Resistance"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
New Techniques in Drug Metabolism Methodology
The title for this session has been taken verbatim from from the title of a presentation by Dr. Donald Hobbs of Pfizer at the first Drug Metabolism GRC, and will provide presentations describing the application of new technologies, such as microfluidics, 3D culture systems and in vitro measurement of protein turnover to improve the mechanistic understanding of drug metabolism and transport to improve in vitro-in vivo extrapolation.
Discussion Leader: Diane Ramsden (Alnylam Pharmaceuticals, United States)
7:30 pm - 7:55 pm
Xiaomeng Shen (Amgen, United States)
"In Vitro Measurement of Target Turnover and Occupancy by IA-LC/MS to Support PK/PD Prediction"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Boyang Zhang (McMaster University, Canada)
"Platform Technology to Increase the Mechanistic Understanding of Drug Transport in Organoids and Engineered Tissues"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Tom Chan (Boehringer Ingelheim Pharmaceuticals, United States)
"Microsomes Bound to Magnetizable Beads: A Novel Format to Study Drug Metabolism"
9:15 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Prediction of Drug Metabolism In Vivo from In Vitro Studies
Fifty years after a presentation with the same title by Dr. Bert LaDu at the first Drug Metabolism GRC, industry, academia and regulatory agencies continue to devote considerable resources to this issue. This session will provide the latest developments in predictive bioinformatic, mathematical modeling and "-omic" approaches by revisiting the contribution of factors like albumin and protein binding, cutting edge technologies like induced pluripotential stem cells and microphysiological systems.
Discussion Leader: Cyrus Khojasteh (Genentech, United States)
9:00 am - 9:30 am
Leslie Benet (University of California, San Francisco, United States)
"IVIVE: Identifying the Unrecognized Unknowns"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Murat Cirit (Javelin Biotech, United States)
"Next-Generation Model Informed Drug Discovery Platform: Merging Microphysiological Systems (MPS) and Quanitative Sytems Pharmacology (QSP)"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Hiroyuki Mizuguchi (Osaka University, Japan)
"In Vitro Models for Drug Metabolism and Response in Poor Metabolizers Using Human iPS Cells and Genome Editing Technology"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Charity Nofziger (PharmGenetix, Austria)
"On Solving the CYP2D6 Incidentalome"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:00 pm - 7:30 pm
Business Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
7:30 pm - 9:30 pm
Selected Poster Presentations
Presentations will be selected from abstracts submitted by graduate students, post-doctoral and early career investigators.
Discussion Leader: Patrick Murphy (Academic Consultant, United States)
7:30 pm - 7:40 pm
Short Talk Selected from Poster Abstracts
7:40 pm - 7:50 pm
Discussion
7:50 pm - 8:00 pm
Short Talk Selected from Poster Abstracts
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:20 pm
Short Talk Selected from Poster Abstracts
8:20 pm - 8:30 pm
Discussion
8:30 pm - 8:40 pm
Short Talk Selected from Poster Abstracts
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:00 pm
Short Talk Selected from Poster Abstracts
9:00 pm - 9:10 pm
Discussion
9:10 pm - 9:20 pm
Short Talk Selected from Poster Abstracts
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Mechanisms of Drug Metabolism
At the first Drug Metabolism GRC in 1971, an entire session was devoted to this topic. In 2022, this session at the 50th anniversary Drug Metabolism GRC will feature cutting edge research in 3D modeling, catalytic cycles, structure-function relationships and related topics.
Discussion Leader: Emily Scott (University of Michigan, United States)
9:00 am - 9:30 am
Xinxin Ding (University of Arizona, United States)
"Bioactivation by P450 Enzymes - Reactive Metabolites, Biomarkers, and Toxic Outcomes"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Ruili Huang (National Center for Advancing Translational Sciences, NIH, United States)
"CYP3A7 Selective Inhibitors and Substrates Identified by High Throughput Screening"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Eric Johnson (Scripps Research, United States)
"Crystal Structures of Drug Metabolizing P450s: Lessons Learned and Applications"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Richard Auchus (University of Michigan, United States)
"Themes and Mechanisms for Steroid Biosynthesis Pathways using Cytochromes P450"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Harnessing Technology to Advance Individualized Therapeutics
This session will describe how advances in modeling and use of biomarkers can facilitate implementation of precision medicine to predict drug disposition and response.
Discussion Leader: Klarissa Jackson (University of North Carolina at Chapel Hill, United States)
7:30 pm - 8:10 pm
Netz Arroyo (Johns Hopkins University School of Medicine, United States)
"Feedback-Controlled Dosing Guided by Real-Time Therapeutic Drug Monitoring"
8:10 pm - 8:30 pm
Discussion
8:30 pm - 9:10 pm
Manthena Varma (Pfizer, United States)
"Scaling Transporter DDIs from In Vitro Findings to the Clinic Via Endogenous Biomarkers and PBPK"
9:10 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure