Study of Erlotinib With or Without Investigational Drug (U3-1287) in Subjects With Advanced Non-small Cell Lung Cancer

Inclusion Criteria

• ≥ 18 years of age.
• Histologically or cytologically confirmed stage IIIB not amenable to surgery or curative intent or stage IV NSCLC.
• Disease progression or recurrence following treatment after last chemotherapy or chemoradiation regimen (completed within the previous 12 months) documented by radiographic assessment.
• Measurable disease by Response Evaluation Criteria for Solid Tumors v1.1 (RECIST v1.1).
• Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
• Adequate bone marrow, renal, and hepatic function.
• Prothrombin time and partial thromboplastin time ≤1.5 x upper limit of normal (ULN).
• Availability of recent (before treatment start) or archival tumor specimens (Phase 2 participants only).
• For female participants, must be postmenopausal, surgically sterile, or must use maximally effective birth control during the period of therapy, and must be willing to use effective contraception up to 6 months after the last dose of study drug and had a negative urine or serum pregnancy test before entry into the study if female participants were of childbearing potential.
• For male participants, must be surgically sterile or willing to use a double barrier contraception method upon enrollment, during the course of the study, and for 6 months following the last investigational drug dose
• Written informed consent.

Exclusion Criteria

• Left ventricular ejection fraction (LVEF) 100 mmHg or systolic > 140 mmHg).
• Clinically significant electrocardiogram changes that obscured the ability to assess the respiratory rate, pulse rate, QT, QTc, and QRS intervals.
• Ascites or pleural effusion requiring chronic medical intervention.
• Myocardial infarction within 1 year before enrollment, symptomatic congestive heart failure (New York Heart Association > Class II), unstable angina, or unstable cardiac arrhythmia requiring medication.
• Treatment with anticancer therapy, antibody based therapy, retinoid therapy, or hormonal therapy within 4 weeks before study treatment or treatment with nitrosoureas or mitomycin C within 6 weeks before study drug treatment or treatment with small molecule tyrosine kinase inhibitors (TKIs) within 2 weeks before study drug treatment. Prior and concurrent use of hormone replacement therapy was permitted.
• Therapeutic radiation or major surgery within 4 weeks before study treatment or palliative radiation therapy within 2 weeks before study drug treatment.
• Participated in clinical drug trials within 4 weeks (2 weeks for small molecule TKIs) before study drug treatment. Current participation in other investigational procedures.
• Uncontrolled infection requiring IV antibiotics, antivirals, or antifungals, known human immunodeficiency virus (HIV) infection, or active hepatitis B or C infection.
• History of hypersensitivity to any of the study drugs or to any excipients.
• Concurrent use of CYP3A4 inducers or inhibitors.
• Any known pre-existing condition including substance abuse that could interfere with participant's participation in and completion of the protocol.