Bioequivalence Study of Trifluridine and Tipiracil Tablets in Colorectal Cancer Patients

Inclusion criteria

• 18-70 years old, life expectancy ≥ 3 months.
• Histologically confirmed colon or rectal adenocarcinoma.
• Has not received anti-tumor therapy before 4 weeks of first dose or Traditional Chinese Medicine anti-tumor therapy before 2 weeks of first dose.
• Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 1.
• Has ability to take oral medication.
• The main organs function are normally, the following criteria are met:

• Hemoglobin (HB) ≥ 100 g / L;
• Absolute neutrophil count (ANC) ≥1.5×109/L;
• Platelets (PLT) ≥ 80 × 109 / L;
• Total serum bilirubin (TBIL) ≤ 1.5 × ULN;
• Alanine transaminase (ALT) and Aspartate aminotransferase (AST) ≤ 2.5 × ULN (when the liver is invaded，AST ≤ 5×ULN);
• Serum creatinine ≤ 132.6 μmol / L.
• Male or female subjects should agree to use an adequate method of contraception starting with the first dose of study therapy through 6 months after the last dose of study (such as intrauterine devices , contraceptives or condoms) ；No pregnant or breastfeeding women, and a negative pregnancy test are received within 7 days before the randomization.
• Understood and signed an informed consent form.

Exclusion criteria

• Has serious diseases , including but not limited to:

• Has diagnosed and/or treated additional malignancy within 5 years prior to randomization. Exceptions include carcinoma in situ of cervix, non-melanoma skin cancer and superficial bladder tumor;
• Has brain metastases;
• Has active infection (such as infection caused body temperature ≥ 38 ° C);
• Has pleural effusion, pericardial effusion, or ascites requiring recurrent drainage before 4 weeks of first dose;
• Has intestinal obstruction, pulmonary fibrosis, renal failure, liver failure or symptomatic cerebrovascular disease;
• Has uncontrolled diabetes (fasting blood glucose (FBG) > 10mmol/L);
• Has myocardial infarction, severe/unstable angina pectoris, New York Heart Association (NYHA) grade III or IV symptomatic congestive heart failure within 12 months prior to first dose;
• Has gastrointestinal bleeding;
• Has HIV infection, or active hepatitis B or C;
• Has a history of organ transplants or autoimmune disease required immunosuppressive therapy;
• Has increased risk associated with participating in the study or taking the study drug, or mental disorders may interfere with the results of the study.
• Has received any of the following treatments before the first dose:

• Has received partial or total gastrectomy;
• Has surgery (such as laparotomy, thoracotomy, and laparoscopic resection of the viscera and/or unhealed wounds) within 4 weeks;
• Has any study drug within 4 weeks.
• Prior therapy with TAS-102.
• Has adverse events caused by previous therapy except alopecia that did not recover to ≤ grade 2.
• Pregnant or lactating woman.
• Subjects who, in the opinion of the investigators, should not participate in the study.