Abstract: Rapid tumor cell growth depends on intracellular polyamine levels higher than those of normal cells. Intracellular polyamine depletion inhibits tumor cell proliferation and induces tumor cell apoptosis. Therefore, polyamine metabolism has recently been identified as an important target for anti-tumor therapy. This article briefly summarizes recent polyamine metabolism targeting, polyamine depletion within the tumor cells through a variety of methods, and the antitumor effects of the treatment.