Triplatin (BBR3464) is a tri-nuclear platinum complex developed by Boehringer Mannheim (now Roche). It is a new-generation platinum chemotherapeutic agent that exhibits cytotoxicity at ten to thousand times lower dose limit compared to the well-known platinum drug cisplatin, in cisplatin-sensitive as well as in cisplatin-resistant cells. DNA is thought to be the primary cellular target of BBR3464. Triplatin is a trinuclear, bifunctional DNA binding agent with an overall charge of 4+, in which the bridging between the two platinating units is made by the [{trans-Pt(NH3)2}m- {H2N(CH2)6NH2}2] linker. This bridging central unit does not contribute to coordinative DNA binding but incorporates into the linker backbone a charge and hydrogen-bonding capacity which dramatically increase the DNA affinity, affect the charge/lipophilicity balance, and further increase the distance between the two Pt–DNA-binding coordination spheres. The predominant DNA adducts of Triplatin are long-range {Pt,Pt} cross-links (CLs) distinctly different from short-range CLs of cisplatin and its mononuclear derivatives. Preclinical studies demonstrated activity in cisplatin-resistant tumours and tumours with mutated p53 status. Phase I & II clinical studies gave preliminary indications of activity in melanoma, pancreatic, lung and ovarian cancers. Triplatin underwent Phase I and II human clinical trials but has not advanced to full use. However, development appears to have been discontinued.