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The effect of acetazolamide (A.A.) on the antineoplastic activity of 1-phthalidyl 5-fluorouracil (PH-FU) against rat and mouse solid tumors was examined. A.A., an inhibitor of liver PH-FU hydrolase, had no antitumor activity but greatly enhanced the activity of PH-FU when coadministered. The potentiation was evaluated in terms of suppression of tumor growth and prolongation of the life-span of tumor-bearing animals. Studies also revealed that A.A. elevated the concentration of PH-FU in tumor tissues, where 5-fluorouracil is slowly liberated from PH-FU. The results are consistent with the hypothesis that A.A. prevents enzymic degradation of PH-FU in the liver and promotes its distribution into target organs.
H Kasai, and
K Tonda, and
M Hirata
August 1985,
Chemical & pharmaceutical bulletin,
H Kasai, and
K Tonda, and
M Hirata
June 1986,
Gan to kagaku ryoho. Cancer & chemotherapy,
H Kasai, and
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M Hirata
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Gan to kagaku ryoho. Cancer & chemotherapy,
H Kasai, and
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M Hirata
December 1984,
Chemico-biological interactions,
H Kasai, and
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October 1982,
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H Kasai, and
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H Kasai, and
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H Kasai, and
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H Kasai, and
K Tonda, and
M Hirata
March 1981,
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H Kasai, and
K Tonda, and
M Hirata
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