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Apaziquone (EOquin) is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases. The active metabolites alkylate DNA and lead to apoptotic cell death. This activity is preferentially expressed in neoplastic cells.
Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan, Inc. for the treatment of superficial (non-muscle invasive) bladder cancer. Approximately 70% of all newly diagnosed patients with bladder cancer have non-muscle invasive bladder cancer and over one million patients in the United States and Europe are affected by the disease. The US Food and Drug Administration (FDA) has granted Fast Track review status to apaziquone for this indication.
- UvA researcher develops new bladder cancer medication. University of Amsterdam, 25 Jul 2007.
- NCI. "apaziquone". Retrieved 2009-06-07.
- Puri, R. et al. Phase I/II Pilot Study of Intravesical Apaziquone (EOquin) for Superficial Bladder Cancer. The Journal of Urology, Volume 176, Issue 4, Pages 1344–1348.
- Hendricksen, K. et al. Safety and Side Effects of Immediate Instillation of Apaziquone Following Transurethral Resection in Patients With Nonmuscle Invasive Bladder Cancer The Journal of Urology, Volume 180, Issue 1, Pages 116–120.
- Puri R, Palit V, Loadman PM; et al. "Phase I/II Pilot Study of Intarvesical Apaziquone (EO9) for Superficial Bladder Cancer". The Journal of Urology (2006) 176 (4):1344-48. Retrieved 2009-06-07.
- FDA Designates Fast Track Status For Apaziquone (EOquin) For Bladder Cancer. Medical News Today, 22 Jul 2009.