A Randomized Phase 2 Trial of TAS-114 in Combination With S-1 Versus S-1

Inclusion Criteria

• Age ≥ 18 years old (≥ 20 years old in Japan);
• Histologically diagnosed or cytologically proven advanced or metastatic NSCLC patients, either Stage IIIB/Stage IV disease (according to Version 7 of the International Association for the Study of Lung Cancer Staging Manual in Thoracic Oncology), or recurrent disease following radiation therapy or surgical resection;
• Patients who had received at least 2 prior therapies for advanced or metastatic disease condition, including platinum doublet and pemetrexed, docetaxel, or immunotherapy, and were refractory to or unable to tolerate their last prior therapy
• Measurable disease as defined by Response Evaluation Criteria in Solid Tumors (RECIST) criteria (Version 1.1, 2009);
• Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1;
• Predicted life expectancy of at least 3 months;
• Able to take medications orally;
• Adequate organ function
• Women of childbearing potential (WOCBP) must have a negative pregnancy test (urine or serum) within 7 days prior to starting the study drug. Both males and females must agree to use effective birth control during the study (prior to the first dose and for 6 months after the last dose) if conception is possible during this interval.
• Willing and able to comply with required scheduled visits and study procedures.

Exclusion Criteria

• Treatment with any of the following within the specified time frame prior to the study drug administration:
• Major surgery within prior 4 weeks and minor surgery within 7 days;
• Radiotherapy for extended field within prior 4 weeks or limited field within prior 2 weeks;
• Any anticancer therapy or investigational agent within prior 3 weeks.
• A serious illness or medical condition
• Concomitant treatment with the following drugs that may interact with S-1:

Sorivudine, brivudine, uracil, eniluracil, folinate/folinic acid, Cimetidine, dipyridamole, and nitroimidazoles, including metronidazole and misonidazoleMethotrexate, Clozapine,Allopurinol,Phenytoin,Flucytosine, a fluorinated pyrimidine antifungal agent,Coumarin-derivative anticoagulant

• Known hypersensitivity to S-1 or its metabolites (eg, 5-FU);
• Previous use of TAS-114, S-1, and 5-FU drugs;
• A pregnant or lactating female or possibly pregnant women, or men or women wishing to have children during the study period;
• A judgment of the investigator that the patient is inappropriate for study participation.