Though rice is the predominant source of energy and micronutrients for more than half of the world population, it does not provide enough zinc (Zn) to match human nutritional requirements. Moreover, climate change, particularly rising atmospheric carbon dioxide concentration, reduces the grain Zn concentration. Therefore, rice biofortification has been recognized as a key target to increase the grain Zn concentration to address global Zn malnutrition. Major bottlenecks for Zn biofortification in rice are identified as low Zn uptake, transport and loading into the grain; however, environmental and genetic contributions to grain Zn accumulation in rice have not been fully explored. In this review, we critically analyze the key genetic, physiological and environmental factors that determine Zn uptake, transport and utilization in rice. We also explore the genetic diversity of rice germplasm to develop new genetic tools for Zn biofortification. Lastly, we discuss the strategic use of Zn fertilizer for developing biofortified rice.