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Cancer encompasses more than 100 diseases with different etiologies and prognoses. According to the latest WHO estimates, the number of cases rose to 18.1 million with 9.6 million deaths. The adoption of strategies to prevent and combat cancer is imperious, including searches for natural products. The mushroom from the Agaricus blazei Murrill species has proven antitumor activity for some types of cancer, and the use of this natural product can improve health and increase the patients' immunity. This paper aimed at researching the molecular mechanisms described in the literature related to antitumor activity and at evaluating possible mechanisms and results associated with the interaction of mushroom extracts with the concomitant use of antineoplastic chemotherapeutic agents and radiotherapy treatment in patients, animal models and in vitro studies. The PubMed, SciELO, Elsevier, and LILACS databases were used as query sources. The studies analyzed confirm that A. blazei presents bioactive molecules with antitumor and antimetastatic activity, involving various biological mechanisms of action. β-glucans are suggested as the main active compounds of the species, whose main biological target is modulation of the immune system. However, the literature provides evidence of several other compounds involved in relevant mechanisms underlying cancer. Evidence on the therapeutic and preventive potential of species A. blazei points to the importance of further studies in order to confirm some discoveries and advance knowledge about mechanisms that can be targets of therapeutic strategies, considering the mushroom as an adjuvant in the treatment and prevention of metastases and deaths.