platinum(iv)-guanidinoneomycin conjugate

A **platinum(iv)-guanidinoneomycin conjugate** is an experimental photoactivatable anticancer prodrug in which a platinum(IV) center is conjugated to guanidinoneomycin, a guanidinium-rich derivative of neomycin[1][2]. The conjugate is designed to improve cell uptake and cancer cell selectivity via the polycationic guanidinoneomycin moiety[1][2]. Upon photoactivation (exposure to visible or UVA light), the platinum(IV) prodrug is reduced to a cytotoxic platinum(II) species that binds and damages DNA, similar to other platinum-based chemotherapies such as cisplatin, but with spatiotemporal control[1][2][9]. The drug is not approved but is studied in vitro for targeted photochemotherapy, showing higher phototoxicity and selectivity for melanoma (SK-MEL-28) cell lines compared to other cancers[1][2]. Its mechanism involves increased intracellular accumulation via guanidinoneomycin, light-triggered reduction of Pt(IV) to active Pt(II), and subsequent DNA binding leading to cell death[1][2][9].

Other names

platinum-guanidinoneomycin conjugateplatinum(iv)-guanidinoneomycin conjugate