Plants have the ability to produce vast amounts of secondary metabolites, including terpenoids, flavonoids, alkaloids, and their derivatives. These metabolites sometimes affect the growth of other organisms, either positively or negatively. Production of defensive compounds, for example phytoalexins, is a well-known strategy used by plants to defend against and withstand invading pathogens. As phytoalexins serve an obvious function in plant defense, they are known as specialized metabolites, substances with a specific biological role that function during specific circumstances. In rice, 15 diterpenoid-type phytoalexins and one flavonoid-type phytoalexin have been identified. Extensive studies have explored the biochemistry, biosynthesis, and biological functions of phytoalexins in rice, specifically the mechanism by which they function in disease resistance. This review focuses on our current knowledge of the transcriptional and hormonal regulation of the production of phytoalexins in rice.