NCIt synonyms : E O9; 3-hydroxymethyl-5-aziridinyl-1-methyl-2-(1H-indole-4,7-dione) prop-beta-en-alpha-ol;
NCIt definition : An indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic
and radiosensitization activities. Apaziquone is converted to active metabolites in
hypoxic cells by intracellular reductases, which are present in greater amounts in
hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell
death. This agent displays selectivity activity towards both hypoxic solid tumors,
which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated
malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase).
Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity.;
Currated CISMeF NLP mapping