Triplatin tetranitrate (rINN; also known as BBR3464, https://www.bioplatinumtech.com/) is a platinum-based cytotoxic drug that underwent clinical trials for the treatment of human cancer.

In preclinical trials it demonstrated cytotoxic activity in cancer cell lines that had either intrinsic or acquired resistance to cisplatin.

Triplatin remains the only “non-classical” platinum drug (not based on the cisplatin structure) to have entered human clinical trials.

More recently, cellular accumulation mediated by heparan sulfate proteoglycans and high-affinity glycosaminoglycan (GAG) binding indicates that cationic PPCs are intrinsically dual-function agents, acting by mechanisms discrete from the neutral, mononuclear agents.

[4] In phase I studies, when given once every 28 days, the main dose-limiting toxicities (DLT) of Triplatin (BBR 3464) were neutropenia and diarrhea encountered at a dose level of 1.1 mg/m2.