Rice (Oryza sativa L.) serves not only as a dietary staple worldwide but also harbours a rich array of bioactive compounds with therapeutic potential. This review explores various therapeutic traits in rice such as phenolic acids, flavonoids, anthocyanins and proanthocyanidins, elucidating their profound health benefits. These compounds act as antioxidants and are crucial in reducing oxidative stress and the risk of type 2 diabetes, obesity, hypertension, high cholesterol, cardiovascular diseases and certain cancers, thereby offering notable nutraceutical benefits. Enhancing these compounds in rice is advantageous, as it is a staple food. The success of crop improvement programs depends on the availability of genetic diversity. This review extensively discusses the genetic diversity among rice genotypes for therapeutic traits and the potential for enhancing these traits through breeding initiatives. Molecular-based approaches are essential in breeding programs, as they enable accurate identification of genetic markers associated with desirable traits and Quantitative Trait Loci (QTLs), facilitating marker-assisted selection easier. These techniques also help to understand the genetic basis and expression of targeted traits. Advances in molecular markers and genomic tools are explored, with an emphasis on developing rice varieties enriched with health-promoting compounds. Furthermore, genome editing and transgenic technologies are examined for their role in precisely modulating bioactive compound levels. This synthesis offers a comprehensive perspective for breeders aiming to enhance therapeutic traits in rice.