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Cancer is one of the major reasons for mortality across the globe. Side effects that are observed with the pharmacological medications present in the market majorly affect the quality of life of patients. This has caused the researchers to find an alternative source of medications such as herbal medicine which has shown a promising effect in anticancer treatment, one such source is Pomegranate, which belongs to the family Punicaceae. Several polyphenols are present in Punica granatum which exhibits properties ranging from antioxidant effect, antidiabetic effect, beneficial impact in treatment, and management of metabolic and cardiovascular disorders to advantageous impact in anticancer treatment. Polyphenols like punicalin, punicalagin, and ellagic acid are a few of the many compounds responsible for the anticancer activity of pomegranate. Many preparations of pomegranate such as Pomegranate Juice (PJ), Pomegranate seed oil (PSO), Pomegranate peel extract (PoPx) etc. are used in various clinical studies. These polyphenols show anticancer activity by either arresting the cell cycle in the G2/M phase, inducing apoptosis, or by damaging the DNA of tumor cells. This review explicitly discusses the role and mechanism of bioactives obtained from the pomegranate in the treatment and management of cancer. The chemical structure, properties and role of pomegranate in the treatment of breast, lung, thyroid, colon, and prostate cancer has been focused in detail. This review also discusses various drug delivery approaches for targeted delivery on tumors as well as patented preparation of pomegranate compounds along with the ongoing clinical trials.