Physiologically based pharmacokinetic (PBPK) modeling, a mathematical modeling approach which uses a pharmacokinetic model to mimick human physiology to predict drug concentration–time profiles, has been used for the discover and development of drugs in various fields, including oncology, since 2000. There have been a few general review articles on the utilization of PBPK in the development of oncology drugs, but these do not include an evaluation of model prediction accuracy. We therefore conducted a systematic review to define the accuracy of PBPK model prediction and its utility throughout all the developmental phases of oncology drugs.