Inclusion Criteria:

- Male or female, aged 18 to 75 years, inclusive

- histologically-confirmed metastatic colorectal carcinoma; measurable lesion according
to the Response Evaluation Criteria in Solid Tumours (RECIST)

- relapsed after treatment with a fluoropyrimidine-based chemotherapy

- prior chemotherapeutic regimen for metastatic or locally advanced disease with an
interval of at least 4 weeks between the last administration of chemotherapy an the
first administration of study treatment

- Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 2

- life expectancy of at least 12 weeks

Exclusion Criteria:

- Known severe hypersensitivity to raltitrexed or any of the excipients of this product

- known severe hypersensitivity to raltitrexed or any of the excipients of this product

- active infection or uncontrolled diarrhoea

- cerebral metastasis or meningeal carcinomatosis

- any evidence of clinically active interstitial lung disease (patients with chronic
stable radiographic changes who are asymptomatic need not be excluded)

- simultaneous antitumoral treatment

- radiotherapy within 2 weeks before entry into the study

- other co-existing malignancies or malignancies diagnosed within the last 5 years with
the exception of basal cell carcinoma or cervical cancer in situ

- any unresolved chronic toxicity greater than common toxicity criteria (CTC) grade 2
from previous anticancer therapy (except alopecia)

- significant clinical disorder or laboratory finding (leukocyte count less than 3.0 x
109 /litre (L) or platelets less than 100 x 109 /L; serum total bilirubin more than
2.0 mg/dl; as judged by investigator, any evidence of severe or uncontrolled systemic
disease (e.g. unstable or uncompensated respiratory, cardiac, hepatic, or renal
disease); creatinine clearance ≥ 65ml/min (according to Cockcroft-Gault formula);
alanine aminotransferase (ALT) or aspartate aminotransferase (AST) greater than 2
times the upper limit of the reference range (ULRR) if no demonstrable liver
metastases, or greater than 5 times the ULRR in the presence of liver metastases)

- pregnancy or breast feeding (women of child-bearing potential)

- concomitant use of phenytoin, carbamazepine, rifampicin, barbiturates, or ST John's
Wort;

- Treatment with a non- approved or investigational drug within 30 days before Day 1 of
study treatment