Arsenic (As) is a metalloid environmental pollutant ubiquitous in nature that causes chronic and irreversible poisoning to humans through its bioaccumulation in the trophic chain. Rice, the staple food crop for 350 million people worldwide, accumulates As more easily compared to other cereal crops due to its growth characteristics. Therefore, an in-depth understanding of the molecular regulatory mechanisms underlying As uptake, transport, and detoxification in rice is of great significance to solving the issue of As bioaccumulation in rice, improving its quality and safety and protecting human health. This review summarizes recent studies on the molecular mechanisms of As toxicity, uptake, transport, redistribution, regulation, and detoxification in rice. It aims to provide novel insights and approaches for preventing and controlling As bioaccumulation in rice plants, especially reducing As accumulation in rice grains.