Drug transporters play an important role in the identification of drug pharmacokinetics. Organic Anion Transport Polypeptide 1B1 / 1B3(OATP1B1 / 1B3) is a transport protein mediating liver absorption of various anionic drugs. The activity of oatp1b1b3 is altered by gene mutations and drug-drug interaction, which can cause serious adverse reactions. In addition to in vitro translation assessment, a DDI risk assessment methodology has been developed. The use of endogenous substrates as probes is an emerging approach to clinically assess the risks of DDI in the early stages of drug development. The pharmacokinetic analysis of the clinical data will then be performed using a physiologic-based pharmacokinetic model to provide a more realistic DDI risk assessment using OATP1B1 / 1B3 substrate drugs. When the drug target is located in Hepatocyte, the effect of INTRAHEPATIC DDI on its pharmacological action is very important. The Positron Emission Tomography allowed the researchers to determine the tissue something concentration time curves of the PET probe after inhibition of oatp1b1b3 and to estimate the kinetic parameters of each intrinsic process of liver clearance of the PET probe. The incorporation of clinical data into the PBPK model allowed a more accurate prediction of the effect of pharmacokinetics on drug delivery and treatment outcomes. The Positron Emission Tomography allowed the researchers to determine the tissue something concentration time curves of the PET probe after inhibition of oatp1b1b3 and to estimate the kinetic parameters of each intrinsic process of liver clearance of the PET probe. The incorporation of clinical data into the PBPK model allowed a more accurate prediction of the effect of pharmacokinetics on drug delivery and treatment outcomes. The Positron Emission Tomography allowed the researchers to determine the tissue something concentration time curves of the PET probe after inhibition of oatp1b1b3 and to estimate the kinetic parameters of each intrinsic process of liver clearance of the PET probe. The incorporation of clinical data into the PBPK model allowed a more accurate prediction of the effect of pharmacokinetics on drug delivery and treatment outcomes.