Dental caries is prevalent, and secondary caries causes restoration failures. This article reviews recent studies on developing a new generation of bioactive resins with anticaries properties. Extensive effects were made to develop new antimicrobial composites, bonding agents, and other resins containing quaternary ammonium methacrylates to suppress plaque buildup and bacterial acid production. The effects of alkyl chain length and charge density and the antimicrobial mechanisms for chlorhexidine, nano-silver, quaternary ammonium methacrylates, and protein-repellent agents were discussed. Synergistic effects of contact-killing and protein-repellent properties were shown to yield the greatest biofilm-inhibition effects. The combination of antimicrobial, protein-repellent, and calcium phosphate nanoparticle remineralization was suggested to provide maximal anticaries effects. In addition, for use orally, cytotoxicity and biocompatibility were important considerations for the new bioactive materials. Furthermore, rather than kill all bacteria, it would be more desirable to modulate the oral biofilm compositions via bioactive resins to suppress cariogenic/pathogenic species and promote benign species. For widespread clinical use of the new antimicrobial and therapeutic materials, whether they would induce bacterial drug resistance needs to be determined, which requires further study. Nonetheless, the new generation of bioactive anticaries resins with therapeutic and biofilm acid-inhibiting properties has the potential to substantially benefit oral health.