We administered pharmacokinetic modulating chemotherapy (PMC, oral tegafur/uracil [UFT] plus fluorouracil infusion) together with irinotecan hydrochloride (CPT-11) in a patient with rectal cancer, who had multiple lung metastases at 2 years and 7 months after surgery. However, because the patient showed resistance, we attempted combination therapy with CPT-11 and doxifluridine (5'-DFUR) on an outpatient basis, which resulted in NC after 9 months. During this period, the therapy was performed safely without any observable adverse reactions such as diarrhea or myelosuppression. This case suggests the efficacy of combination therapy with CPT-11 and 5'-DFUR, which was expected since this is an established treatment for progressive recurrent colon cancer.