A review of the use of cisplatin in cancer chemotherapy in humans is presented. The emphasis is placed on the chemistry, in vivo distribution and biotransformation of this agent. The existing literature pertinent to the physicochemical properties of cisplatin and structure activity relationships of platinum coordination complexes is reviewed. The chemistry of this drug, both in aqueous media and in biological systems is discussed as well as current analytical methodology used for monitoring 'cisplatin levels' in biological fluids. Recent advances in analytical methodology specific for cisplatin are also presented and recent findings in the area of the possible biotransformations of this important anticancer agent are discussed.