CONSPECTUS: Formation of iodinated disinfection byproducts (I-DBPs) in drinking water has become an emerging concern. Compared to chlorine-and bromine-containing DBPs, I-DBPs are more toxic, have different precursors and formation mechanisms, and are unregulated. In this Account, we focus on recent research in the formation of known and unknown I-DBPs in drinking water. We present the state-ofthe-art understanding of known I-DBPs for the six groups reported to date, including iodinated methanes, acids, acetamides, acetonitriles, acetaldehyde, and phenols. I-DBP concentrations in drinking water generally range from ng L −1 to low-μg L −1 . The toxicological effects of I-DBPs are summarized and compared with those of chlorinated and brominated DBPs. I-DBPs are almost always more cytotoxic and genotoxic than their chlorinated and brominated analogues. Iodoacetic acid is the most genotoxic of all DBPs studied to date, and diiodoacetamide and iodoacetamide are the most cytotoxic. We discuss I-DBP formation mechanisms during oxidation, disinfection, and distribution of drinking water, focusing on inorganic and organic iodine sources, oxidation kinetics of iodide, and formation pathways. Naturally occurring iodide, iodate, and iodinated organic compounds are regarded as important sources of I-DBPs. The apparent second-order rate constant and half-lives for oxidation of iodide or hypoiodous acid by various oxidants are highly variable, which is a key factor governing the iodine fate during drinking water treatment. In distribution systems, residual iodide and disinfectants can participate in reactions involving heterogeneous chemical oxidation, reduction, adsorption, and catalysis, which may eventually affect I-DBP levels in finished drinking water. The identification of unknown I-DBPs and total organic iodine analysis is also summarized in this Account, which provides a more complete picture of I-DBP formation in drinking water. As organic DBP precursors are difficult to completely remove during the drinking water treatment process, the removal of iodide provides a cost-effective solution for the control of I-DBP formation. This Account not only serves as a reference for future epidemiological studies to better assess human health risks due to exposure to I-DBPs in drinking water but also helps drinking water utilities, researchers, regulators, and the general public understand the formed species, levels, and formation mechanisms of I-DBPs in drinking water.