To Determine the MTD and to Evaluate the Safety, Efficacy and PK Profiles of TSB-9-W1 in Pre-treated Patients With mCRC.

Inclusion Criteria:

1. Female or male, age ≥ 20 years old
2. Patient who is eligible and able to participate in the study and accepts to enter the study by signing written informed consent
3. Patient has histologically or cytologically confirmed colorectal adenocarcinoma in stage IV under the Tumor-Node-Metastasis (TNM) staging system
4. Patient must have at least one measurable lesion according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1
5. Patient should have received at least two prior therapies for colorectal cancer (CRC) including oxaliplatin and irinotecan based regimens.
6. Patient should have received at least one of the target therapies for CRC including Cetuximab, Bevacizumab, Panitumumab, Regorafenib, and Ziv-aflibercept.
7. Patient with primary major surgery needs to have elapsed ≥ 2 weeks prior to the planned first study treatment day
8. Patient who has ever received chemotherapy, or immunotherapy, or biologic therapy modalities need to wash-out ≥ 2 weeks prior to the baseline visit
9. Patient who has ever received radiotherapy (including chemoradiation therapy) need to end the course ≥ 2 weeks before baseline visit (palliative radiotherapy can be performed on non-study-related local lesions)
10. Patient's life expectancy ≥ 3 months
11. Within 4 weeks of planned first study treatment day, adequate hematopoietic functions are presented:

    * Total white blood cell (WBC) ≥ 3,000 cells/mm3
    * Absolute neutrophil count (ANC) ≥ 1,500 /mm3
    * Hemoglobin (Hb) ≥ 9.0 g/dL
    * Platelets ≥ 100,000 cells/mm3
12. Within 4 weeks of planned first study treatment day, adequate hepatic and renal functions (AST: aspartate aminotransferase, ALT: alanine aminotransferase, ALP: alkaline phosphatase) are presented:

    * Total bilirubin ≤ 2.0 mg/dL
    * AST ≤ 3 x ULN; liver metastasis patients: AST ≤ 5 x ULN
    * ALT ≤ 3 x ULN; liver metastasis patients: ALT ≤ 5 x ULN
    * ALP ≤ 5 x ULN
    * Creatinine ≤ 1.5 mg/dL
13. Eastern Cooperative Oncology Group (ECOG) performance score ≤ 2
14. Patient can take food and drug orally
15. Male and female patients should use appropriate contraception method(s) shown below during the study and at least 2 weeks after the end of treatment for female patients.

    * Total abstinence (when this is in line with the preferred and usual lifestyle of the subject. Periodic abstinence (e.g., calendar, ovulation, symptothermal, post-ovulation methods) and withdrawal are not acceptable methods of contraception).
    * Female sterilization (have had surgical bilateral oophorectomy with or without hysterectomy) or tubal ligation at least six weeks before taking study treatment. In case of oophorectomy alone, only when the reproductive status of the woman has been confirmed by follow up hormone level assessment.
    * Male sterilization (at least 6 months prior to screening). For female subjects on the study, the vasectomized male partner should be the sole partner for that subject
    * Combination of any two of the following (a+b or a+c, or b+c):

      1. Use of oral, injected or implanted hormonal methods of contraception or other forms of hormonal contraception that have comparable efficacy (failure rate \<1%), for example hormone vaginal ring or transdermal hormone contraception.
      2. Placement of an intrauterine device (IUD) or intrauterine system (IUS).
      3. Barrier methods of contraception: Condom or Occlusive cap (diaphragm or cervical/vault caps) with spermicidal foam/gel/film/cream/vaginal suppository.

Exclusion Criteria:

1. Patient who has participated in other investigational studies within 4 weeks prior to the first dose of the study medications
2. Patient has history of another malignancy within 5 years prior to study entry, except curatively treated non-melanoma skin cancer, or cervical cancer in situ
3. Patient with known or suspected hypersensitivity to TSB-9-W1 or its formulation excipients
4. Patient has another severe and/or life-threatening medical disease
5. Patient has immuno-compromised condition, with known autoimmune conditions or human immunodeficiency virus (HIV) seropositivity
6. Patient with active systemic infections, active and clinically significant cardiac diseases, clinically active gastroduodenal ulcers, or medical conditions that may significantly affect adequate absorption of investigational product
7. Patient with known brain metastasis
8. Patient with medical, social or psychological factors interfering with compliance
9. Patient having grade ≥ 3 adverse event (AE) based on National Cancer Institute - Common Terminology Criteria for Adverse Event (NCI-CTCAE) 4.03 except blood total bilirubin, AST, ALT, ALP and creatinine at baseline visit
10. Patient having grade ≥ 1 diarrhea based on NCI-CTCAE 4.03.
11. Patient with a medical history of myocardial infraction in the last 6 months