Several snake toxins are widely studied due to their broad therapeutic potential. The venom produced by snakes of the genus Crotalus sp presents a wide variety of pharmacological uses of its isolated fractions, such as antifungal, antiviral, antibacterial, and antitumor properties, among other therapeutic potentialities. Regarding its antitumor action, this venom has a direct effect on tumor cells, and the isolation of its compounds is important for the characterization of the anticarcinogenic actions. Toxins derived from snake venoms have proven to be excellent biological tools to evaluate the inhibition of metastasis in vitro and in vivo, as well as the direct action on tumor cells. Crotalus durissus terrificus venom and its toxins have been widely evaluated as potential candidates for the development of new antineoplastic therapies, efficient against different tumor lines and cellular targets. This work highlights this snake’s venom toxins, focusing on the antineoplastic properties.