The purpose of this study is to evaluate the dose-limiting toxicity (DLT), toxicity profile, maximum tolerated dose (MTD) and characterize the pharmacokinetics of biweekly PEP02 treatment.

Inclusion Criteria:

• Histopathologically confirmed metastatic colorectal cancer
• Documented disease progression after first-line chemotherapy containing oxaliplatin
• Both genders, age 18 years
• ECOG performance status 0 or 1
• Adequate organ and marrow function
• Written informed consent to participate in the study

Exclusion Criteria:

• Have received irinotecan treatment
• With active CNS metastases (indicated by clinical symptoms, cerebral edema, steroid requirement, or progressive growth)
• With clinically significant gastrointestinal disorder (e.g. bleeding, inflammation, obstruction, including partial or complete obstruction secondary to peritoneal carcinomatosis, or diarrhea > grade 1)
• With uncontrolled intercurrent illness that could limit study compliance considered to be ineligible for the study by the investigators including, but NOT limited to, any of the following:ongoing or active infection requiring antibiotic treatment, symptomatic congestive heart failure, unstable angina pectoris, or cardiac arrhythmia psychiatric illness or social situation that would preclude study compliance
• With other primary malignancies, except those remain disease-free for 3 or more years after curative treatment.
• Prior chemotherapy within 3 weeks
• Major surgery or radiotherapy within 4 weeks
• Prior participation in any investigational drug study within 3 weeks
• History of allergic reaction to liposome product
• Pregnant or breastfeeding (a urine pregnancy test must be performed on all patients who are of childbearing potential before entering the study, and the result must be negative)