Provided herein are methods, compositions and kits for the treatment of locally advanced or metastatic breast cancer or breast cancer brain metastases. The method comprises administration of 4-iodo-3-nitrobenzamide, a metabolite or salt thereof in combination with irinotecan. The method of treating locally advanced or metastatic breast cancer comprises at least one 21 day treatment cycle.本明細書において、イリノテカンと組み合わせた4-ヨード-3-ニトロベンズアミド、その代謝産物又はその薬学的に許容しうる塩の投与を含む、乳癌を治療するための方法及び組成物が提供される。