Study of TAS-102 in Patients With Metastatic Colorectal Cancer Refractory to Standard Chemotherapies

This is a multinational, double-blind, two-arm, parallel, randomized Phase 3 comparison study
evaluating the efficacy and safety of TAS-102 versus placebo in patients with refractory
metastatic colorectal cancer. Patients will be randomly assigned (2:1) to TAS-102
(experimental arm) or placebo (control arm).

Inclusion Criteria:

1. Has provided written informed consent

2. Has adenocarcinoma of the colon or rectum

3. Has failed at least 2 prior regimens of standard chemotherapies for metastatic
colorectal cancer

4. ECOG performance status of 0 or 1

5. Is able to take medications orally

6. Has adequate organ function (bone marrow, kidney and liver)

7. Women of childbearing potential must have a negative pregnancy test and must agree to
adequate birth control if conception is possible. Males must agree to adequate birth
control.

Exclusion Criteria:

1. Certain serious illnesses or medical condition(s)

2. Has had certain other recent treatment e.g. major surgery, anticancer therapy,
extended field radiation, received investigational agent, within the specified time
frames prior to study drug administration

3. Has received TAS-102

4. Has unresolved toxicity of greater than or equal to CTCAE Grade 2 attributed to any
prior therapies

5. Is a pregnant or lactating female