A cancer therapeutic agent according to the present invention comprises a combination of compound A described below, or a pharmaceutically acceptable salt thereof, and compound B described below, or a pharmaceutically acceptable salt thereof: Compound A: compound A1 represented by formula (1) below, or water-soluble prodrug A2 thereof; Compound B: at least one type of compound selected from the group consisting of a platinum-type anticancer compound, a gemcitabine-type compound, a 5-FU-type compound, a taxane-type compound, a vinca alkaloid-type compound, an anticancer tyrosine kinase inhibitor compound, and an anticancer monoclonal antibody; ##STR00001## (wherein, R.sup.11 represents a hydrogen atom, a halogen atom or a C1-C6 alkyl group;R.sup.12 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or a hydroxyl group;R.sup.21 represents a hydrogen atom or a C1-C10 alkyl group which may comprise one to three substituents selected from Group B described below: Group B: a C1-C6 alkoxy group, a hydroxy group, a halogen atom, an amino group, a mono-C1-C6 alkylamino group, a di-C1-C6 alkylamino group, a C3-C7 cycloalkyl group, a heterocycle, and an aryl ring (the aryl ring may comprise one to three substituents selected from the group consisting of a hydroxy group, a C1-C6 alkoxy group, a halogen atom, an amino group, a mono-C1-C6 alkylamino group, and a di-C1-C6 alkylamino group); andR.sup.22 represents a hydrogen atom, an amino group, or a C1-C6 alkyl group that may comprise one to three substituents selected from Group C described below, a C1-C6 alkoxy group that may comprise one to three substituents selected from Group C described below, a C1-C6 alkylthio group that may comprise one to three substituents selected from Group C described below, a mono-C1-C6 alkylamino group that may comprise one to three substituents selected from Group C described below, or a di-C1-C6 alkylamino group that may comprise one to three substituents selected from Group C described below: Group C: a C1-C6 alkoxy group, a hydroxy group, a halogen atom, an amino group, a C3-C7 cycloalkyl group, a heterocycle, and an aryl ring (the aryl ring may comprise one to three substituents selected from the group consisting of a hydroxy group, a C1-C6 alkoxy group, an amino group, a mono-C1-C6 alkylamino group, and a di-C1-C6 alkylamino group).

 
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