A Platinum(IV) ProdrugPerfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain

Effective delivery to the brain limits the development of novel glioblastoma therapies. Here, we introduce conjugation between platinum­(IV) prodrugs of cisplatin and perfluoroaryl peptide macrocycles to increase brain uptake. We demonstrate that one such conjugate shows efficacy against glioma stem-like cells. We investigate the pharmacokinetics of this conjugate in mice and show that the amount of platinum in the brain after treatment with the conjugate is 15-fold greater than with cisplatin after 5 h.