Mechanism of action of cis-dichlorodiammineplatinum(II).

Although the mechanism of action of cis-dichlorodiammineplatinum(II) is not definitely known, much has been discovered regarding its antitumor effect. Although neutral in plasma, the platinum complex becomes aquated intracellularly to form a positively charged platinum species that is likely to interact with nucleophilic sites. The purine and pyrimidine bases of DNA possess such sites and provide the locale for the majority of the biologically effective intracellular platinum binding. Although several types of binding are possible, the biologically important lesions are most likely interstrand and/or intrastrand cross-links. The extent of formation and the rate of cellular repair of these lesions may determine the ultimate effect of cis-dichlorodiammineplatinum(II) on the cell.