A pharmaceutical composition for cancer treatment and the applications are disclosed. The pharmaceutical composition and a kit strengthen the anti-cancer effects of Capecitabine and reduce side effects. The pharmaceutical composition comprises an effective dose of Capecitabine with an anti-cancer effect, an effective dose of Gimeracil with an anti-cancer synergy, and an effective dose of Oteracil potassium capable of reducing side effects, and is used to treat cancers of mammals which are sensitive to 5-Fluorouracil.