This systematic review aims to determine the potential of bioactive compounds present in Balatinaw rice (Oryza sativa) extracts against the formation of cancer and aims to prove the promising bioactivity of Oryza sativa extract as medicinal plant. Cancer is an uncontrolled proliferation of aberrant cells in different parts of the body. The cancerous cells continuously replicate and replace the normal tissues. These changes of normal tissue into abnormal tissue can result in death and this is one of the most concerning causes of death in today’s time. The Balatinaw rice (Oryza sativa) is a valuable natural resource that contains active chemical compounds, and it is one of the largest and most important staple food crops. This can aid in the development of a therapeutic drug and reduce the risk of certain disease such as cancer, diabetes, and cardiovascular disease. All chosen journals that were considered were thoroughly investigated and passed the systematic review criteria; 11 eligible journals from 2014 to present were utilized. The results show that Oryza sativa carries a bioactive compound which are the phenolic and flavonoid compounds. These two have a major role in minimizing the risks of inflammatory disorders. From the eleven (11) articles that were reviewed, six (6) of them present ferulic, p-coumaric acid, and gallic acid which were consistent to have in rice bran. All the three pigmented rice types have the reduction capacity in the viability of the following cancer cell lines. Also, studies have shown that the present phenolic and flavonoid compound in Oryza sativa extract has the capability to inhibit cancer cell proliferation and metastasizes while triggering apoptosis. Moreover, the phenolic and flavonoid compounds revealed a significant property, cytotoxic properties, which can stimulate cytolytic and antiproliferative to cancer cells. In conclusion, the biochemical activity of flavonoid and phenolic compounds present in Oryza sativa extract can be utilized as a therapeutic treatment against various cancers and considered as cheap and effective treatment.