The Discovery and Development of Cisplatin

728 Journal of Chemical Education • Vol. 83 No. 5 May 2006 • www.JCE.DivCHED.org The discovery of the anticancer activity of cisplatin {cis[PtCl2(NH3)2]} in the 1960s and its subsequent clinical success generated interest in the use of metal compounds in cancer treatment (1, 2). Thousands of platinum compounds have since been prepared and evaluated as potential chemotherapeutic agents, although few have entered clinical use (3, 4). Worldwide annual sales of platinum-based anticancer drugs are currently of the order of two billion U.S. dollars (5, 6). Several other metal compounds have been found to display promising anticancer activity including a variety of complexes of ruthenium and gold as well as metallocenes of Ti, Nb, Mo, and Re (2). The platinum(II) drugs, carboplatin {cis[Pt(NH3)2(CBDCA)], CBDCA = 1,1-cyclobutanedicarboxylic acid} and oxaliplatin {[Pt(oxalato)(1R,2R-chxn)], chxn = cyclohexane-1,2-diamine}, have also entered the clinic, supplementing and complementing cisplatin. Cisplatin is responsible for the cure of over 90% of testicular cancer cases and it plays a vital role in the treatment of cancers such as ovarian, head and neck cancer, bladder cancer, cervical cancer, melanoma, lymphomas, as well as several others (3, 4, 7, 8).