Inclusion Criteria:

1. Provide signed and dated informed consent prior to study-specific screening
procedures

2. ≥ 18 years old

3. Histologically or cytologically confirmed inoperable locally advanced or metastatic
(stage IIIB/IV) NSCLC

4. ≥ one prior chemotherapy regimen (including adjuvant chemotherapy)(not to have
included erlotinib or other EGFR inhibiting agent)

5. Measurable disease as defined by Response Evaluation Criteria in Solid Tumors
(RECIST)

6. Eastern Cooperative Oncology Group (ECOG) performance status 0 to 1

7. Male or female patients of child-producing potential must agree to use double barrier
contraception, oral contraceptives or avoidance of pregnancy measures during the
study and for 90 days after the last day of treatment

8. Females of childbearing potential must have a negative serum pregnancy test

9. Good organ function

10. Confirmed availability of archival pathology samples (10 unstained paraffin-embedded
slides) or tissue block suitable for subsequent analysis of KRAS, EGFR, and c-Met

Exclusion Criteria:

1. Previous receipt of erlotinib or other EGFR inhibiting therapy

2. Receipt of any anti-tumor treatment for NSCLC within 4 weeks (2 weeks for
radiotherapy) prior to the start of designated treatment

3. Documented major surgical procedure within 4 weeks prior to randomization.

4. Symptomatic central nervous system metastases either considered in the opinion of
investigator to be clinically unstable or which require steroids, anti-epileptics, or
other symptom-relieving medications

5. Pregnant, breast-feeding, or refusing double barrier contraception, oral
contraceptives or avoidance of pregnancy measures

6. Significant gastrointestinal disorder that, in opinion of Investigator, could
interfere with the absorption of ARQ 197 and/or erlotinib (e.g. Crohn's disease,
small or large bowel resection, malabsorbtion syndrome)

7. Unable or unwilling to swallow the complete dose of erlotinib or ARQ 197

8. Any known contraindication to treatment with ARQ 197 or erlotinib

9. Any known hypersensitivity to any of component of ARQ 197 or erlotinib

10. Other malignancy within 5 years of randomization, with the exception of adequately
treated intraepithelial carcinoma of the cervix uteri, prostate carcinoma with a PSA
value < 0.2 ng/ml or basal or squamous cell carcinoma of the skin

11. Previously diagnosed grade 3 or 4 (CTCAE) bradycardia or other heart arrhythmia

12. Any other significant co-mormid condition that, in opinion of the Investigator, would
impair study participation or cooperation

13. Known human immunodeficiency virus (HIV), hepatitis B virus (HBV) or hepatitis C
virus (HCV) infection