Inclusion Criteria:

- Men or women age ≥18 years

- Histologically or cytologically confirmed NSCLC (Recurrent, locally advanced or
metastatic, inoperable NSCLC [Stage IIIB/IV]. Patients with Stage IIIB NSCLC must
have a cytologically documented pleural effusion.)

- Failed or relapsed after receiving a platinum-containing chemotherapy regimen as
first-line therapy for advanced NSCLC

- Measurable disease on computerized tomography (CT) scan

- ECOG Performance Status of 0 or 1

- Expected survival ≥12 weeks

- Provide written informed consent

Exclusion Criteria:

- More than 2 prior chemotherapy regimens

- Progression of disease on prior pemetrexed treatment

- Brain metastases (exception: patients who had a resection and/or completed a course
of cranial irradiation, have no worsening CNS symptoms, and have discontinued all
corticosteroids for that indication for at least 1 month)

- Serum creatinine ≥2.0mg/dL or creatinine clearance <45mL/min

- Absolute neutrophil count <1500/μL or platelets <100,000/μL

- Any malignancy within 5 years immediately prior to the first dose of study medication
(exception: basal cell or non-metastatic squamous cell carcinoma of the skin, and
carcinoma in-situ of the cervix)

- Any comorbidity or condition which, in the opinion of the investigator, may interfere
with the assessments and procedures of this protocol

- Patients who are within 28 days of chemotherapy, radiation therapy, immunotherapy, or
investigational medication for NSCLC. Patients must have recovered from all of the
side effects of treatment.

- Pregnancy or lactation. Women of childbearing potential and non-vasectomized men must
agree to use a barrier method of contraception during treatment.