PtIV56-5FUMeOBut

PtIV56-5FUMeOBut is a novel multimechanistic fluorouracil-platinum(IV) prodrug designed to overcome resistance in colorectal cancer models. It is synthesized by coordinating a derivative of the antimetabolite 5-fluorouracil (5FU) to a platinum(IV) complex derived from the cytotoxic platinum(II) precursor PtII56MESS (also known as 56MESS). The prodrug is designed to be reduced intracellularly, releasing both the active platinum(II) species and 5FU. This dual-action approach combines the DNA-binding cytotoxicity of the platinum complex with the DNA synthesis-disrupting activity of 5FU. Preclinical studies have demonstrated that PtIV56-5FUMeOBut exhibits enhanced cellular uptake and potency against cisplatin-resistant colorectal cancer cells, effectively inducing apoptosis and increasing reactive oxygen species production.