Disinfection of drinking water is recognized as a principal public health triumph of the 20th Century, as it significantly reduced waterborne illness and increased life expectancy. However, an unintended consequence was the generation of disinfection byproducts (DBPs) that are formed by the reaction of disinfectants with natural and anthropogenic organic matters. Epidemiological studies have suggested an association of the long-term exposure to drinking water DBPs with increased adverse reproductive outcomes and colorectum and bladder cancers. Nitrogenous DBPs have attracted increasing attention in recent years because, compared to carbonaceous DBPs, they generally possess higher genotoxicity, cytotoxicity, and carcinogenicity. This project aims to review the formation pathways of nitrogenous DBPs in drinking water to provide a comprehensive understanding of their formation mechanism and potential impacts on public health. Our enhanced knowledge is expected to guide future studies on effectively reducing their formation and subsequently mitigating their potential health risks.