Mark R Albertella, Paul M Loadman, Philip H Jones, Roger M Phillips, Roy Rampling, Neil Burnet, Chris Alcock, Alan Anthoney, Egils Vjaters, Chris R Dunk, Peter A Harris, Alvin Wong, Alshad S Lalani, Chris J Twelves
PURPOSE: AQ4N is a novel bioreductive prodrug under clinical investigation. Preclinical evidence shows that AQ4N penetrates deeply within tumors and undergoes selective activation to form AQ4, a potent topoisomerase II inhibitor, in hypoxic regions of solid tumors. This proof-of-principle, phase I study evaluated the activation, hypoxic selectivity, and safety of AQ4N in patients with advanced solid tumors. EXPERIMENTAL DESIGN: Thirty-two patients with cancer (8 glioblastoma, 9 bladder, 8 head and neck, 6 breast, and 1 cervix) received a single 200 mg/m(2) dose of AQ4N before elective surgery...
February 15, 2008: Clinical Cancer Research