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The use of whole body physiological‐based pharmacokinetic (PBPK) models linked with in vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has become embedded within many of the pharmaceutical industry and is used even as part of regulatory submissions. These include the influence of transporter proteins on drug disposition, a subject for which we have witnessed an increasing awareness. A combination of the development of high‐powered analytical techniques and antibody‐based technology, together with a realization that an understanding of absolute transporter protein abundances together with activity can potentially enhance the modelling of transporter kinetics by PBPK–IVIVE link models. This review summarizes the mechanistic approaches to integrate suitable non‐biased in vitro transporter kinetic data relevant to the intestine (i.e. ‘intrinsic’ K_i, ‘intrinsic’ K_m), by in …