Considering minimally invasive dentistry, recent restorative materials are expected to provide a therapeutic effect on the remaining tooth structure. Using inert restorations which lack interaction between restorative materials and tooth structure is not satisfactory nowadays. This has shifted the focus in biomaterial sciences towards innovative bioactive restorative materials that can remineralize remaining tooth structures and provide healing and protective properties. Understanding the remineralization process of demineralized dentine and the mechanism by which these bioactive materials potentially repair these tissues, will provide room for future advancements and clinical applications in restorative dentistry. This article provides a review of the basic dentine structure, the caries process, and different dentine remineralization models. Also, it details various bioactive materials with an understanding of their main classification in terms of remineralization potential.