Primary human hepatocytes are widely used to study drug metabolism and enzyme induction. However, primary hepatocytes rapidly lose their hepatic function in conventional 2D cultures. Recently, a microphysiological system that overcomes this drawback has been actively investigated and applied in drug discovery research. Such novel in vitro models are desirable for the evaluation of the metabolic clearance of drugs with low turnover, drug-induced liver injury, and chronic liver diseases like liver fibrosis. This article reviews the characteristics and recent advances in 3D-bioprinted human liver tissue models in drug discovery research.