Abstract: Traditional cell models and animal models have certain limitations in simulating the complexity and physiological relevance of human tissues, thereby limiting both the efficiency of clinical translation and the predictive performance of physiologically based pharmacokinetic models. Organoids and organ-on-a-chip technologies, as emerging tools in drug research, more closely mimic in vivo physiological processes and can simulate the complex mechanical environments and physiological responses of the body. This article reviews the research progress of organoids and organ-on-a-chip for physiologically based pharmacokinetic modeling, demonstrating the potential of this combination to facilitate the translation from preclinical research to the clinical stage and to improve predictive capability, thereby providing new perspectives for drug development and assessment.