PtIVP-5FUMeOBut

PtIVP-5FUMeOBut is a novel fluorouracil-platinum(IV) prodrug designed as a multimechanistic chemotherapeutic agent. It is synthesized by derivatizing the antimetabolite 5-fluorouracil (5FU) and coordinating it to a platinum(IV) complex derived from the platinum(II) precursor PtIIPHENSS. This dual-action design aims to overcome drug resistance, particularly in cisplatin-resistant colorectal cancer, by combining the DNA synthesis-disrupting activity of 5FU with the DNA-damaging cytotoxicity characteristic of platinum-based agents. Preclinical studies have demonstrated its potential through enhanced cellular uptake and cytotoxicity in colorectal cancer models, including 3D spheroid cultures, while inducing apoptosis and affecting mitochondrial membrane potential.