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apaziquone

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Also known as EOQUIN

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.

Wikidata facts

Mass
288.111
Has use
medication
Show 4 more facts
chemical formula
C₁₅H₁₆N₂O₄
subject has role
antineoplastic
isomeric SMILES
CN1C(=C(C2=C1C(=O)C=C(C2=O)N3CC3)CO)/C=C/CO
canonical SMILES
CN1C(=C(C2=C1C(=O)C=C(C2=O)N3CC3)CO)C=CCO
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Encyclopedic overview

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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.

Excerpted from Wikipedia’s “apaziquone” article, available under the CC BY-SA 4.0 licence.

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