Inclusion Criteria:

- Signed Informed Consent Form(s)

- Histologically confirmed NSCLC

- Recurrent or progressive disease after receiving at least one chemotherapy regimen
for advanced or metastatic NSCLC

- Eastern Cooperative Oncology Group (ECOG) performance status 0, 1, or 2

- Age ≥ 18 years

- Recovery from reversible acute effects of prior anti-cancer therapy (chemotherapy,
radiotherapy, or investigational treatment) to NCI Common Toxicity Criteria for
Adverse Events (NCI CTCAE) Grade ≤ 1 (excluding alopecia)

- Ability to comply with the study and follow-up procedures, including all specified
imaging studies

- Ability to take oral medication

- Availability of archival diagnostic paraffin-embedded tumor tissue and willingness to
provide sufficient tissue for testing for EGFR levels in tumor by both
immunohistochemistry (IHC) and fluorescence in situ hybridization (FISH)

- Life expectancy ≥ 3 months

- Measurable disease on computed tomography (CT)

- At least one detectable lesion on FDG-PET scan and/or FLT-PET scan that is measurable
on CT

- Use of an acceptable means of contraception (men and women of childbearing potential)
or documentation of infertility

Exclusion Criteria:

- Prior treatment with an investigational or marketed agent for the purpose of
inhibiting epidermal growth factor receptor (EGFR) (including, but not limited to,
erlotinib and gefitinib)

- Chemotherapy, radiotherapy, or investigational treatment within 14 days or within 5
half-lives of the active molecules in the chemotherapy or investigational treatment,
whichever is longer, prior to study entry or from which patients have not yet
recovered

- Inability to take oral medications, disease affecting gastrointestinal absorption, or
prior surgical procedure affecting gastrointestinal absorption

- Uncontrolled diabetes

- Any unstable systemic disease (including active infection, unstable angina,
congestive heart failure, myocardial infarction within 1 month prior to study entry,
hepatic, renal, or metabolic disease)

- Pregnancy or lactation

- History of another malignancy in the past 2 years, unless the malignancy has been
adequately treated, is currently not detectable, and is associated with a 5-year
survival > 90%

- Claustrophobia

- Any other disease, condition, physical examination finding, or clinical laboratory
finding which, in the opinion of the investigator, makes the patient inappropriate
for the study