Guadecitabine is a dinucleotide antimetabolite consisting of decitabine linked via a phosphodiester bond to deoxyguanosine, with antineoplastic activity. Upon metabolic activation, cleavage of the phosphodiester bond allows incorporation of decitabine into DNA, inhibiting DNA methyltransferase and inducing genome-wide hypomethylation and S-phase cell cycle arrest. The compound is resistant to cytidine deaminase, leading to gradual release of decitabine both extracellularly and intracellularly, resulting in prolonged exposure.
