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Apaziquone
Chemical compound
Chemical compound
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Apaziquone (tentative trade name EOquin) is an indolequinone that is a bioreductive prodrug similar to 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 apoptosis. This activity is preferentially expressed in neoplastic cells.
After administration of apaziquone directly into the urinary bladder (intravesically), the drug and its active metabolite were not detected in plasma, and there were no systemic side effects.
Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan for the treatment of superficial (non-muscle invasive) bladder cancer. In 2016, FDA issued a complete response letter informing the company that its new drug application for apaziquone in bladder cancer would not be approved.
References
References
- (25 Jul 2007). "UvA researcher develops new bladder cancer medication". University of Amsterdam.
- NCI. "apaziquone".
- (October 2006). "Phase I/II pilot study of intravesical apaziquone (EO9) for superficial bladder cancer". J. Urol..
- (July 2008). "Safety and side effects of immediate instillation of apaziquone following transurethral resection in patients with nonmuscle invasive bladder cancer". J. Urol..
- (22 Jul 2009). "FDA Designates Fast Track Status For Apaziquone (EOquin) For Bladder Cancer". Medical News Today.
- (18 Nov 2016). "FDA Issues Complete Response Letter for Apaziquone in Bladder Cancer". OncLive.
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