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: Quantitative Extrapolations of Transporters and Drug Metabolizing Enzymes
Discussion Leader: Donavon McConn (Takeda San Diego, USA)
7:40 pm - 7:55 pm
Opening Remarks
7:55 pm - 8:55 pm
Joseph Polli (GlaxoSmithKline, Inc., USA)
"A Quantification Identity Crisis for DMPK and ADME-Exploring Advances in Quantitative Predictions of Drug Metabolism, Transport, Safety and Pharmacokinetics"
8:55 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
Quantitative Predictions for Non-P450 Mechanisms
Discussion Leader: Tom Leyh (The Albert Einstein College of Medicine, USA)
9:00 am - 9:05 am
Introduction by Discussion Leader
9:05 am - 9:30 am
Hansruedi Glatt (Federal Institute for Risk Assessment, Germany)
"Role of Sulfotransferases in Metabolic Activation"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Wen Xie (University of Pittsburgh, USA)
"Sulfotransferases in Liver Disease"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
S. Joshua Swamidass (Washington University in St. Louis, USA)
"Modeling the In Vivo Balance Between Phase I and Phase II Metabolism"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Barry Potter (University of Oxford, United Kingdom)
"Sulfatase Inhibitors: From Concept to Clinic and Beyond"
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
Antibody/ADC Biophysics Considerations in Predicting
Human Disposition
Discussion Leader: Brooke Rock (Amgen, USA)
7:30 pm - 7:35 pm
Introduction by Discussion Leader
7:35 pm - 7:55 pm
Jun Wu (Amgen, USA)
"Binding Affinity of LM to FcRn and Its Importance in Disposition of Large Molecules"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Mengmeng Wang (Pfizer, USA)
"Understanding Localization of Biotherapeutics at Whole body, Tissue and Cellular Level in Preclinical Development"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Denise O'Hara (Pfizer, USA)
"Physiologically-Relevant Kd Measurements to Inform PK-PD Modeling"
9:15 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Safety Considerations in Clinical Drug Metabolism and Transport
Discussion Leader: Maciej Zamek-Gliszczynski (GlaxoSmithKline, USA)
9:00 am - 9:05 am
Introduction by Discussion Leader
9:05 am - 9:30 am
Kunal Taskar (GlaxoSmithKline, United Kingdom)
"Pharmacokinetics, Efficacy and Safety in Drug-Drug Interactions: Do They Go Hand in Hand?"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Xiaoyan Chu (Merck & Co., Inc., USA)
"Understanding Complex Perpetrator DDIs Involving Hepatic/Gut Transporters and Their Interplay with CYP3A Enzymes: From In Vitro to Mechanistic Clinical Evaluations"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Adrian Ray (Gilead Sciences, Inc., USA)
"Thiamine Transporters: Emerging Mechanisms of Drug Toxicity and Disposition"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Mary Paine (Washington State University, USA)
"Identification of Natural Products as Precipitants of Clinical Drug Interactions: Challenges and Opportunities"
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
Challenging Michaelis-Menten Drug Metabolism
and Transport Kinetics
Discussion Leader: Christopher Kemper (Pharma Navigators, LLC, USA)
7:30 pm - 7:35 pm
Introduction by Discussion Leader
7:35 pm - 7:55 pm
Kenneth Korzekwa (Temple University, USA)
"Using Numerical Approaches to Model Complex CYP Kinetics"
7:55 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
Rory Remmel (University of Minnesota, USA)
"Atypical Kinetics of UDP-Glucuronosyltransferases: The Problem of Determining Accurate In Vitro Clearances"
8:35 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Joanne Wang (University of Washington, USA)
"Atypical Kinetics in Drug Transporters: Theoretical and Practical Considerations"
9:15 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Quantitative Understanding of Fraction Metabolized: Newer Challenges in Scaling and Predictivity
Discussion Leader: Griff Humphreys (Bristol-Myers Squibb, USA)
9:00 am - 9:05 am
Introduction by Discussion Leader
9:05 am - 9:35 am
Philip Potter (St. Jude Children's Research Hospital, USA)
"Evaluating In Vivo Esterase-Mediated Drug Metabolism: Should Be Easy, but Why Do We Fail?"
9:35 am - 9:50 am
Discussion
9:50 am - 10:15 am
Yurong Lai (Gilead Sciences, USA)
"The Combination of Bottom-Up and Top-Down Modelling Approaches to Predict In Vivo Hepatic Uptake Clearance and Tissue Partitioning"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Bhagwat Prasad (University of Washington, USA)
"Role of Quantitative Proteomics Data to Predict Fraction Metabolized by Non-CYP Enzymes"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Birk Poller (Novartis Pharma AG, Switzerland)
"ECM-Based IVIVE Method for the Prediction of Human Clearance and Relative Elimination Pathway Contributions"
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
Young Investigator Presentations
Six poster abstracts from trainees will be highlighted with short oral presentations.
Discussion Leader: Patrick Murphy (Academic Consultant, USA)
7:30 pm - 7:45 pm
Theresa Aliwarga (University of Washington, USA)
"Formation and Distribution of Cis- and Trans-Epoxyeicosatrienoic Acids in Patients with Cardiovascular Disease"
7:45 pm - 7:50 pm
Discussion
7:50 pm - 8:05 pm
Laura Doyle (University of Kansas, USA)
"Treatment of Hepatocellular Carcinoma HepG2 Cells with β-Naphthoflavone Simultaneously Increased Intracellular and Exosomal Expression of CYP1A1"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:25 pm
Gassiot Matthieu (Institut de Recherche en Cancérologie de Montpellier (IRCM), U1194, INSERM, France)
"Identification of Molecular Determinants Involved in the Transport and Metabolism of Kinase Inhibitors in Prostate Cancer Cells"
8:25 pm - 8:30 pm
Discussion
8:30 pm - 8:45 pm
Luc Rougee (Eli Lilly and Company, USA)
"Time-Dependent Inhibition of Cytochrome P450 3A4 by Itraconazole and Metabolites"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:05 pm
Kimberly Holt (Temple University School of Pharmacy, USA)
"Comparison of Different Tissue:Plasma Water Partition Coefficient Models and Their Ability to Predict the Steady-State Volume of Distribution and the Concentration-Time Profiles in Humans"
9:05 pm - 9:10 pm
Discussion
9:10 pm - 9:25 pm
Deepak Kumar Bhatt (University of Washington, USA)
"Genetic Variation, Age, and Gender Are Associated with Human Liver UGT2B17 Protein Abundance and Activity"
9:25 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Emerging Technologies in Predicting Extrahepatic Metabolism and Toxicity
Discussion Leader: Rheem Totah (University of Washington, USA)
9:00 am - 9:05 am
Introduction by Discussion Leader
9:05 am - 9:30 am
Murat Cirit (Massachusetts Institute of Technology, USA)
"Translational Applications of the Human Physiome on a Chip"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Kelsey Retting (Organovo, USA)
" A Three-Dimensional Bioprinted Model of the Renal Proximal Tubule for Evaluation of Drug-Induced Nephrotoxicity"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Kevin Healy (University of California, Berkeley, USA)
"Microphysiological Organ Systems for Drug Discovery, Disease Modeling, Personalized Medicine"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Elizabeth Gillam (University of Queensland, Australia)
"Ancestral Sequence Reconstruction of P450s: the 'Retro' Approach to Understanding Drug Metabolism"
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
Advances and Challenges in Predicting Human PK Profiles
Discussion Leader: Natalie Hosea (Global DMPK, Takeda California, USA)
7:30 pm - 7:35 pm
Introduction by Discussion Leader
7:35 pm - 8:00 pm
Neil Parrott (Roche, Switzerland)
"Physiologically-Based Pharmacokinetic (PBPK) Modeling Predictions for Entry into Human (EIH) Studies: An Analysis of Small Molecule Development Candidates at Hoffmann-LaRoche, 2003-2015"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:35 pm
J. Cory Kalvass (AbbVie, USA)
"Assessment of Dose, Intrinsic Pharmacokinetics, and Efficacious Steady-State Concentration of 368 Oral Drugs"
8:35 pm - 8:45 pm
Discussion
8:45 pm - 9:10 pm
Tristan Maurer (Pfizer, USA)
"Early
PK Predictions to Enable Rational and Efficient Drug Design"
9:10 pm - 9:20 pm
Discussion
9:20 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure