Antimony, a natural element that has been used as a drug for over more than 100 years, has remarkable therapeutic efficacy in patients with acute promyelocytic leukemia. This review focuses on recent advances in developing antimony anticancer agents with an emphasis on antimony coordination complexes, Sb (III) and Sb (V). These complexes, which include many organometallic complexes, may provide a broader spectrum of antitumoral activity. They were compared with classical platinum anticancer drugs. The review covers the literature data published up to 2007. A number of antimonials with different antitumoral activities are known and have diverse applications, even though little research has been done on their possibilities. It might be feasible to develop more specific and effective inhibitors for phosphatase-targeted, anticancer therapeutics through the screening of sodium stibogluconate (SSG) and potassium antimonyltartrate-related compounds, which are comprised of antimony conjugated to different organic moieties. For example, SSG appears to be a better inhibitor than suramin which is a compound known for its antineoplastic activity against several types of cancers.