Abstract: P-glycoprotein(P-gp)is an important efflux protein of ATP-binding cassette transporter superfamily. Cells could be protected from detrimental xenobiotics by the up-regulation of efflux pumps. In this review, an extensive literature search for P-gp induction research was conducted, and a focus was brought onto the P-gp induction models, experiment methods and its applications in drug discovery. We mainly introduced the in vitro cell-based models and in vivo rodent animal models for induction research, methods that investigate induction potency by detecting the protein, gene expression and efflux function, as well as co-regulation between P-gp and other transporters or drug metabolism enzymes. P-gp induction can serve as a clinical therapeutic strategy by reducing the intracellular concentration of deleterious xenobiotics significantly, and the in silico P-gp induction pharmacophore model was also discussed. This review could be of great importance for pre-clinical drug design, the screening of new synthesized compounds and the prediction of potential clinical drug-drug interactions.