Characterization of variability in drug disposition is important for clinical study design and individualized drug treatment. As variability in drug disposition cannot be completely described by genetics, characterization of phenotypic variability is critical. This has fostered the development of plasma-derived exosomes as liquid biopsy and endogenous biomarkers for the prediction of drug metabolism and transport. Integration of metabolomics and proteomics data into physiologically-based pharmacokinetic models also supports data translational for better prediction of drug disposition. This symposium will provide an update on various non-invasive and in silico approaches to drive the prediction of in vivo drug disposition.