Phase I Primary Objective:

• Determine the MTD of Aroplatin/capecitabine subjects with unresectable local recurrence or distant metastases of colorectal cancer refractory to 5-FU/LV and irinotecan.

Phase II Primary Objective:

• Evaluate the response proportion and duration with Aroplatin/capecitabine therapy.

Phase II Secondary Objective:

• Evaluate the frequency of adverse events.

Inclusion criteria:

• Histologically confirmed colorectal cancer: unresectable local recurrence or distant metastases;
• Measurable disease (RECIST criteria);
• Refractory to 5-FU / leucovorin and irinotecan as described below;
• No prior therapy with oxaliplatin, any other platinum or capecitabine;
• ECOG score 0-2 (Karnofsky 100-70%);
• Life expectancy of greater then or equal to 5 months;
• Adequate hematopoietic, liver and renal function;
• Women of child-bearing potential have to practice adequate contraception;
• Signed written informed consent;
• Subjects must be willing to be followed during the course of treatment/observation and follow-up.

Refractory metastatic colorectal cancer

The following subjects are regarded refractory to treatment:

• Those with progression while receiving 5-FU/LV/irinotecan;
• Those with progression on irinotecan after prior 5-FU/LV treatment;
• Progression within six months of adjuvant 5-FU/LV/irinotecan;
• Progression within six months of adjuvant 5-FU/LV followed by progression on irinotecan

Subjects must have received at least one or more commonly used 5-FU/leucovorin and irinotecan regimens. Prior adjuvant therapy is allowed including 5-FU/leucovorin or other fluoropyrimidines except capecitabine and irinotecan.

Exclusion criteria:

• Previously diagnosed brain metastases if symptomatic and requiring active therapy;
• Other cancers within the last five years, with the exception of adequately treated cone-biopsied in situ carcinoma of the cervix uteri or basal or squamous cell carcinoma of the skin;
• Concurrent chemotherapy or immunotherapy;
• Prior therapy for colorectal cancer within one month of admission to the present study;
• Primary or secondary immunodeficiency or use of corticosteroids or other immunosuppressive medication;
• Any serious concomitant medical or mental illness requiring intense therapy and interfering with participation in this study;
• Women must not be pregnant or breast-feeding;
• No participation in any clinical trial involving investigational drugs within 1 month from enrollment into the present study.