Increasingly sophisticated, powerful in vitro and in vivo models are being developed for drug discovery and development, which are complex to understand or master for the average users. Thus, the objective of this symposium is to bring experts on the generation and utility of such in vitro and in vivo models together to present the latest developments, discuss potential pitfalls and challenges, and showcase successful applications of the models in drug discovery and development research, driving appreciation for novel approaches and perhaps new collaborations.