Method for Reducing Gastrointestinal Toxicity Due to the Administration of Tegafur

A method for treating cancer in a mammal wherein the cancer is susceptible to 5-fluorouracil therapy, the method comprising simultaneously administering to the mammal a therapeutically effective amount of tegafur, 2,4-dihydroxy-5-chloropyridine in an amount effective for potentiating the antitumor effect of tegafur, and oxonic acid or a pharmaceutically acceptable salt thereof in an amount effective for suppressing gastrointestinal toxicity, under fasting conditions.

A method for inhibiting inflammation and gastrointestinal toxicity caused by the administration of tegafur, comprising administering oxonic acid or a pharmaceutically acceptable salt thereof in an amount effective for suppressing gastrointestinal toxicity, simultaneously with said tegafur to a patient in need of such treatment, wherein said tegafur and oxonic acid or a pharmaceutically acceptable salt thereof are administered under fasting conditions.

A method for decreasing the breakdown of oxonic acid in the gastrointestinal tract of a patient undergoing treatment with tegafur, comprising administering oxonic acid simultaneously with said tegafur to said patient under fasting conditions.

A kit for treating cancer in a mammal, comprising tegafur, 2,4-dihydroxy-5-chloropyridine, oxonic acid or a pharmaceutically acceptable salt thereof in dosages suitable for administration twice a day, and optionally comprising an anti-tumor agent selected from the group consisting of cisplatin, 1,3-bis(2-chloroethyl)-1-nitrosourea, docetaxel, doxorubicin, epirubicin, etoposide, methotrexate, mitomycin, gemcitabine, carboplatin, gefitinib, pemetrexed, Avastin, Cetuximab and paclitaxel, the kit further comprising an indicator that reminds that said tegafur, said 2,4-dihydroxy-5-chloropyridine, and said oxonic acid or a pharmaceutically acceptable salt thereof should be administered under fasting conditions.

A pharmaceutical composition for potentiating the antitumor effect of tegafur while reducing gastrointestinal toxicity in a patient in need of such treatment, comprising (A) a therapeutically effective amount of tegafur, (B) a dihydropyrimidine dehydrogenase inhibitor in an amount effective for potentiating the antitumor effect and (C) oxonic acid or a pharmaceutically acceptable salt thereof in an amount effective for suppressing gastrointestinal toxicity, and optionally an additional anti-tumor agent selected from the group consisting of cisplatin, 1,3-bis(2-chloroethyl)-1-nitrosourea, docetaxel, doxorubicin, epirubicin, etoposide, methotrexate, mitomycin, gemcitabine, carboplatin, gefitinib, pemetrexed, Avastin, Cetuximab and paclitaxel, the pharmaceutical composition being contained in a package that comprises an indicator that reminds the patient that the pharmaceutical composition should be administered under fasting conditions.