Pathway for Biomarkers of Transporter Inhibition as a Replacement for Clinical Drug-Drug Interaction Studies

Session Description

Clinical evidence supports inhibition of key hepatic and renal uptake transporters as important mechanisms of DDIs with potential alterations in drug safety and efficacy. Past characterization of such DDIs has often required conduct of individual clinical studies to assess interactions between the inhibitor NME and a sensitive/selective substrate probe drug. However, recent drug outcome or transporter genotype studies has delineated attractive associations of transporters with endogenous substrates. This session will provide insight on state-of-the-art application and strategies in which specific biomarkers have emerged as promising clinical translated predictors of DDIs, will provide examples of practical drug development applications to reduce DDI risk, and discuss knowledge gaps that restrict the validation of biomarkers to replace traditional transporter DDI studies.

Learning Objectives

1. Recognize the most promising endogenous biomarkers of transporter inhibition that have emerged from clinical translation to drug-drug interaction (DDI) studies.

2. Appraise knowledge gaps of biomarker validation and translation to replace traditional drug probe substrate DDI studies.

Session Schedule

12:15 PM - 12:17 PM ET
Opening Remarks
Caroline A. Lee, PhD and Jason Sprowl, PhD

12:17 PM - 12:37 PM ET
State-of-the-Art in Clinical Validation of Transporter Inhibition Biomarkers, Translation to Predict DDIs with Substrate Drugs and Use of Genotypes to Validate Endogenous Substrates
Kathleen Giacomini, PhD

12:37 PM - 12:57 PM ET
OATP1B Biomarkers: Selectivity, Sensitivity and Applications in Drug Development
Xiaoyan Chu, PhD

12:57 PM - 1:02 PM ET
Regulatory Perspective on Biomarkers
Xinning Yang, PhD

1:02 PM - 1:15 PM ET
Live Q&A
All Speakers