Inclusion Criteria:

- Pathological proven diagnosis of NSCLC with positive EGFR status by
immunohistochemistry. Patients will be considered as positive if greater than 10% of
the tumor cells are positively stained by the EGFR pharmDX assay kit.

- Disease that is locally advanced, metastatic, or recurrent.

- Prior treatment with 1 or 2 chemotherapy regimens, including a platinum based regimen
for advanced disease (stage IIIB with malignant pleural effusion or stage IV).

- Evidence of unidimensionally measurable disease as per Response Evaluation Criteria
in Solid Tumors [RECIST].

- Radiographic evidence of disease progression during or following previous
chemotherapy treatment.

- Formalin fixed, paraffin embedded tumor tissue from the initial diagnoses will be
obtained.

- Male or female, 19 years of age or older.

- ECOG performance status 0 2.

- Resolution of all acute toxic effects of prior therapy or surgical procedures (except
for alopecia).

- Bisphosphonate therapy for bone metastases is allowed; however, treatment must be
initiated prior to the first dose of therapy. Prophylactic use of bisphosphonates in
patients without bone disease, except for the treatment of osteoporosis, is not
permitted.

- Ability to swallow and retain oral medication.

- Adequate organ function as defined by the following criteria:

- Hemoglobin >9.0 g/dL.

- Absolute neutrophil count (ANC) >1500/μL.

- Platelet >100,000/μL.

- Serum creatinine <1.75 × ULN.

- Serum albumin >3.0 g/dL.

- Total serum bilirubin <1.5 × ULN.

- Serum aspartate transaminase (AST) and serum alanine transaminase (ALT) <2.5 ×
ULN, or AST and ALT <5 × ULN if liver function abnormalities are due to
underlying malignancy

- Signed and dated informed consent indicating that the subject (or legally acceptable
representative) has been informed of all pertinent aspects of the trial prior to
enrollment.

- Willingness and ability to comply with scheduled visits, treatment plans, laboratory
tests, and other study procedures.

- Males and non-pregnant, non-lactating females age 19 years or older.

Exclusion Criteria:

- Prior treatment with >2 systemic chemotherapy based regimens for advanced disease
(stages IIIB/IV).

- Prior treatment with any EGFR inhibitors (TK inhibitor or monoclonal antibody).

- Symptomatic brain metastases or spinal cord compression; subjects will be eligible
after adequate treatment (radiotherapy, surgery) and having stable disease not
requiring steroids.

- Diagnosis of any second malignancy within the last 3 years, except basal cell
carcinoma, squamous cell skin cancer, or in situ carcinoma that has been adequately
treated.

- Any significant acute or chronic medical (e.g., gastrointestinal complications,
myocardial infarction, unstable angina, congestive heart failure, cerebrovascular
accident, infection, metabolic complications, etc.) or psychiatric conditions that
would impart, in the judgment of the investigator, excess risk associated with study
participation, or study drug administration.

- Known human immunodeficiency virus (HIV) infection.

- Current treatment on other therapeutic clinical trials.

- Known hypersensitivity to gossypol, its enantiomers, or its excipients.

- Any other condition or circumstance that would, in the opinion of the Investigator,
make the patient unsuitable for participation in the study.

- Patients with symptomatic hypercalcemia or hypercalcemia that is > grade 2.

- Patients with malabsorption syndrome, disease significantly affecting
gastrointestinal function, or resection of the stomach or small bowel are excluded.
Subjects with ulcerative colitis, inflammatory bowel disease, or partial or complete
small bowel obstruction are also excluded.

- Pregnancy or breastfeeding. Female patients must be surgically sterile or be
postmenopausal, or must agree to use effective contraception during the period of
therapy. All female patients with reproductive potential must have a negative
pregnancy test within 3 days prior to enrollment. Male patients must be surgically
sterile or must agree to use effective contraception during the period of therapy.