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 Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
Keynote Session: Drug Metabolism in the Multiverse of Discovery
Discussion Leader: Mitchell Taub (Boehringer Ingelheim Pharmaceuticals, 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
Donglu Zhang (Genentech, United States)
"New Lessons From The Biotransformation and Distribution of ADCs, PROTACs, and Small Molecules"
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
Targeted Protein Degraders: Route-Dependent Absorption Considerations and Other Determinants of Successful Matchmaking
Discussion Leader: Sara Humphreys (Amgen, United States)
9:00 am - 9:30 am
Keith Hornberger (Arvinas, Inc., United States)
"Innovative Approaches to Understanding PROTAC Oral Absorption"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Chonghui Gu (Foghorn Therapeutics, United States)
"Long Acting Injectable Formulation as a Drug Delivery Platform for Protein Degrader"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
David Belair (AbbVie, United States)
"Mechanistic Modeling for Targeted Protein Degradation: Absorption, Cellular Uptake, and IVIVC"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Mark Niosi (Pfizer, United States)
"In Vitro Methods to Predict Degrader Intestinal Absorption"
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.
Organizer: Leslie Dickmann (University of Wisconsin-Madison, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Novel Mechanisms and Methods to Predict Drug Interactions
Discussion Leader: Michael Mohutsky (Eli Lilly and Company, United States)
7:30 pm - 7:55 pm
Jaydeep Yadav (Merck, United States)
"Use of Modeling Approaches for Evaluating Time Dependent Inhibition Mediated Drug-Drug Interactions"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Luc Rougee (Eli Lilly and Company, United States)
"Getting it Right: How In Vitro Conditions Alter CYP Inhibition"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Joanne Wang (University of Washington, United States)
"Improving Drug-Drug Interaction Predictions for Renal OCT2 and MATE1/2-K Transporters: Impact of Inhibitor Intracellular Accessibility and Flux Studies in a Double Transfection System"
9:15 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Approaches, Interpretations, and Applications of Fraction Unbound
Discussion Leader: Robert Jones (Genentech, Inc., United States)
9:00 am - 9:30 am
Li Di (Pfizer, United States)
"Impact of Plasma Protein Binding on Pharmacokinetics and Drug-Drug Interaction"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
J. Cory Kalvass (AbbVie, United States)
"Experimental and Kinetic Considerations for Interpreting Drug Unbound Fraction: Free Drug Hypothesis Implications and Caveats"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Jashvant (Jash) Unadkat (University of Washington, United States)
"Does Albumin Facilitate Transporter-Mediated Uptake Clearance of OATP Drugs?"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Late-Breaking Topic
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
Sex, Gender, and ADME Science
Discussion Leader: Valerie Kramlinger (Vanderbilt University, United States)
7:30 pm - 7:55 pm
Robert Bies (University at Buffalo, United States)
"PBPK Models of the Female Reproductive Tract: Prediction of Plasma and Local Tissue Concentrations After Drug Administration"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Melanie Nicol (University of Minnesota, United States)
"Hormones, Microbes, and Drugs in the Female Genital Tract: Models to Address the Enigma"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Lauren Cirrincione (University of Washington, United States)
"Applying Clinical Pharmacology to Transgender Medicine"
9:15 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Technologies for Translational DMPK
Discussion Leader: Tom Chan (Boehringer Ingelheim Pharmaceuticals, United States)
9:00 am - 9:30 am
Danilo Tagle (NCATS, NIH, United States)
"Microphysiological Systems: Complex In Vitro Platforms for Safety, Efficacy and Disease Models for Precision Medicine"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Jose Ayuso (University of Wisconsin, United States)
"The Role of Microfluidics and Microphysiological Systems in Drug Metabolism"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Salman Khetani (University of Illinois Chicago, United States)
"Normal and Diseased Engineered Liver Platforms for Investigating Drug Disposition"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Bingming Chen (Merck, United States)
"From Molecules to Visuals: Empowering Drug Discovery and Development with Mass Spectrometry Imaging"
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
Early-Career Investigator Presentations
Discussion Leaders: Swati Nagar (Temple University, United States) and Kim Brouwer (University of North Carolina (UNC) Eshelman School of Pharmacy, United States)
7:30 pm - 7:45 pm
Short Talk Selected from Poster Abstracts
7:45 pm - 7:50 pm
Discussion
7:50 pm - 8:05 pm
Short Talk Selected from Poster Abstracts
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:25 pm
Short Talk Selected from Poster Abstracts
8:25 pm - 8:30 pm
Discussion
8:30 pm - 8:45 pm
Short Talk Selected from Poster Abstracts
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:05 pm
Short Talk Selected from Poster Abstracts
9:05 pm - 9:10 pm
Discussion
9:10 pm - 9:25 pm
Short Talk Selected from Poster Abstracts
9:25 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Business Meeting
Nominations for the Next Vice Chair(s); Complete the GRC Evaluation Forms; Discuss Future Dates and Venue; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Structures and Mechanisms of Metabolizing Enzymes and Transporters
Discussion Leader: D. Fernando Estrada (University at Buffalo, SUNY, United States)
9:00 am - 9:30 am
Simone Brixius-Anderko (University of Pittsburgh, United States)
"Of HETEs and HEMEs - Targeting Cytochrome P450 Fatty Acid Hydroxylases to Treat Human Disease"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Ute Hellmich (Friedrich Schiller University Jena, Germany)
"Fun with Fluorine: Following and Fiddling with Drug/Protein Complex Formation"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Manish Shah (Albany College of Pharmacy and Health Sciences, United States)
"Structural Biology of Human CYP2C9 and CYP2C8: Impact of Genetic Polymorphisms and Ligand Binding"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Edward Yu (Case Western Reserve University, United States)
"Structure of the Plasmodium Falciparum NCR1 Transporter"
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
Tracking Missing Metabolites
Discussion Leader: Donglu Zhang (Genentech, United States)
7:30 pm - 7:55 pm
Klarissa Jackson (University of North Carolina at Chapel Hill, United States)
"Missing Metabolites Implicated in Drug-Induced Liver Injury"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Chungang (Chuck) Gu (Biogen Inc., United States)
"Radiolabel to Uncover "Missing" Metabolites of Candidate Drugs"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Cyrus Khojasteh (Genentech, United States)
"Understanding Missing Metabolites in Drug Metabolism by Unlocking Complexity"
9:15 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure