The compound cis-[Pt(NH)Cl] was first described by Italian chemist Michele Peyrone in 1845, and known for a long time as Peyrones salt. The structure was deduced by Alfred Werner in 1893. In 1965, Barnett Rosenberg, Van Camp et al. of Michigan State University discovered that electrolysis of platinum electrodes generated a soluble platinum complex which inhibited binary fission in Escherichia coli (E. coli) bacteria. Although bacterial cell growth continued, cell division was arrested, the bacteria growing as filaments up to 300 times their normal length. The octahedral Pt(IV) complex cis-[PtCl(NH)], but not the trans isomer, was found to be effective at forcing filamentous growth of E. coli cells. The square planar Pt(II) complex, cis-[PtCl(NH)] turned out to be even more effective at forcing filamentous growth. This finding led to the observation that cis'-[PtCl(NH)] was indeed highly effective at regressing the mass of sarcomas in rats. Confirmation of this discovery, and extension of testing to other tumour cell lines launched the medicinal applications of cisplatin.  Cisplatin was approved for use in testicular and ovarian cancers by the U.S. Food and Drug Administration on 19 December 1978. and in the UK (and in several other European countries) in 1979. 
Cisplatin was the first to be developed. 
In 1983 pediatric oncologist Roger Packer began incorporating cisplatin into adjuvant chemotherapy for the treatment of childhood medulloblastoma. The new protocol that he developed led to a marked increase in disease-free survival rates for patients with medulloblastoma, up to around 85%. The Packer Protocol has since become a standard treatment for medulloblastoma. Likewise, cisplatin has been found to be particularly effective against testicular cancer, where its use improved the cure rate from 10% to 85%.
Recently, some researchers have investigated at the preclinical level new forms of cisplatin prodrugs in combination with nanomaterials in order to localize the release of the drug in the target.