Worldwide, cancer is a great cause of death and a public health issue. Cancer has been the leading cause of death in developing nations for many years. Cancers are typically treated with surgery, immunotherapy, chemotherapy, and radiation therapies. However, these techniques have some undesirable side effects, including neurological illness, high toxicity levels, discomfort, and mental stress. Biologically active compounds discovered in mushrooms may be utilized to reduce ill effects and increase the efficacy of the current therapies. Mushrooms have efficient therapeutic activities such as antimicrobial, antitumor, antidiabetic, anticancer, and antioxidant activity. Bioactive compounds like polysaccharides, terpenoids, β-glucan, steroids, polyphenols, flavonoids, proteins, and peptides have precisely well-recognized anticancer activity. In this review paper, we described the biomedical activities of the mushroom against various cancers. The immune-modulating components in mushrooms activate NK cells and macrophages to target cancer cells. Due to immunomodulatory properties of mushroom-derived bioactive compounds in cancer therapy to highlight the need for further research in this area further studies needs to validate in clinical samples.