Drinking water disinfection is crucial for the elimination of pathogens and the prevention of waterborne diseases. However, this process also results in the formation of numerous disinfection byproducts (DBPs). Toxicological research has shown that DBPs can adversely influence living organisms, and epidemiological studies suggest that consuming disinfected drinking water may increase health risks. However, the toxicity of disinfected drinking water remains unclear due to the wide variety of DBP species and the complex nature of DBP toxicity. Therefore, deciphering the toxicity of DBPs is crucial for reducing the health risks associated with drinking water disinfection. In this review, we summarize recent studies focusing on the toxicity effects of DBPs at various biological levels, including individual level, cellular level, and genetic level. Given the current state of research, this review outlines progress and advancements while also discussing existing challenges and future directions in this field.