Introduction: Accurate prediction of pharmacokinetic (PK) and toxicokinetics (TK) of drugs is imperative for successful development of new pharmaceutics. Although conventional in vitro methods for predicting the PK and TK of drugs are well established, limitations still exist and more advanced chip-based in vitro platforms combined with mathematical models can help researchers overcome the limitations. Areas covered: We will review recent progress in the development of multi-organ-on-a-chip platforms for predicting PK and TK of drugs, as well as mathematical approaches that can be combined with these platforms for experiment design, data analysis and in vitro-in vivo extrapolation (IVIVE) for application to humans. Expert opinion: Although there remain some challenges to be addressed, the remarkable progress in the area of multi-organ-on-a-chip in recent years indicate that we will see tangible outcomes that can be utilized in the pharmaceutical industry in near future.
Keywords: Multi-organ-on-a-chip; pbpk model; pharmacodynamic; pharmacokinetic; toxicokinetic.