Figure 1From: PR-104 a bioreductive pre-prodrug combined with gemcitabine or docetaxel in a phase Ib study of patients with advanced solid tumours Chemical structures of PR-104 and its biotransformation products. PR-104 undergoes rapid hydrolysis by systemic phosphatases to PR-104A that becomes activated by NADPH-cytochrome P450 oxidoreductases and other one-electron reductases in hypoxia, or in oxic conditions by AKR1C3, to reactive nitrogen mustards that crosslink DNA causing tumour cytotoxicity. PR-104 is metabolically deactivated by glucuronidation or N-dealkylationBack to article page