Inclusion Criteria:

1. Age ≥ 20 years.

2. Diagnosed stage III/IV NSCLC. The grading is determined according to the
Tumor-Node-Metastasis (TNM) staging system for lung cancer.

3. Patients with histologically or cytologically proven primary NSCLC with
adenocarcinoma or mixed cell type with adenocarcinoma, who have failed on standard
treatments.

4. With progressive tumor after two lines of chemotherapy (including one platinum-based)
and 1 EGFR-targeted therapy if patient is identified with EGFR mutation or his/her
EGFR mutation status is unknown OR having refused further currently approved
treatment modalities.

5. Life expectancy ≥ 3 months.

6. Within 1 week of planned first study treatment day, adequate hematopoietic functions
are presented: Total white blood cell (WBC) ≥ 3500 cells/mm3 Hemoglobin (Hb) ≥ 9.0
g/dL Platelets ≥ 100,000 cells/mm3 Absolute neutrophil count (ANC) ≥ 1500 /mm3

7. Within 1 week of planned first study treatment day, adequate hepatic and renal
functions are presented: Total bilirubin ≤2.0 mg/dLGOLANTA20090911, Amendment 4/v.
1.0/ 13 October 2010 AST ≤ 3 × upper limit of normal (ULN); patients with liver
metastasis: AST ≤ 5 × ULN ALT ≤ 3 × ULN; patients with liver metastasis: ALT ≤ 5 ×
ULN Creatinine ≤ 1.5 mg/dL

8. Must have recovered from toxicities of previous anti-cancer treatments to grade 1
NCI-CTC or better, except for alopecia.

9. Eastern Cooperative Oncology Group (ECOG) performance score ≤ 2.

10. Female patient with childbearing potential confirmed of not being pregnant at the
screening; and informed that effective contraception must be used during the entire
treatment period of this study and for 6 months after exiting from the study.

11. Given signed and dated written informed consent form.

Exclusion Criteria:

1. Primary major surgery < 4 weeks prior to the planned first study treatment day.

2. Lactating, pregnant or plans to be become pregnant.

3. Except for alopecia, recovered from any previous treatments to a grade 1 or less
prior to the planned first study treatment day.

4. With active systemic infections, active and clinically significant cardiac diseases,
active gastrointestinal ulcers, or medical conditions that may significantly affect
adequate absorption of investigational product.

5. Within 5 years, prior history of malignancy other than NSCLC, except cervical
carcinoma in situ and basal or squamous cell skin carcinoma.

6. Known allergic to antroquinonol or its formulation excipients.

7. Within 14 days of planned first study treatment day, exposed to any drug(s) known to
be significant CYP2C19, 3A4, 2C8, and 2E1, inhibitor or activator.

8. With conditions judged by the investigator as unsuitable for the study.