A Phase 1/2 Trial of Enzastaurin and Erlotinib in Patients With Advanced Solid Tumors and Non-Small Cell Lung Cancer (NSCLC) After Prior Chemotherapy

Inclusion Criteria:

1. Phase 1: Any incurable solid malignancy, with no more than 3 prior systemic treatment
regimens.

Phase 2: Histologic diagnosis of advanced NSCLC, Stage IIIB with malignant pleural
effusion or Stage IV per American Joint Committee on Cancer Staging Criteria for
NSCLC. Patients must have failed 1 or 2 prior systemic treatment regimen(s).

2. Performance status of 0, 1, or 2 on the Eastern Cooperative Oncology Group (ECOG)
Scale

3. Prior chemotherapy must be completed at least 2 weeks prior to study enrollment, and
the patient must have recovered from acute toxic effects (except alopecia) prior to
enrollment.

4. Prior radiotherapy is allowed to < 25% of the bone marrow Prior radiotherapy must be
completed at least 2 weeks before study enrollment, and the patient must have
recovered from acute toxic effects (except alopecia) prior to enrollment.

5. Non-measurable or measurable disease as defined by RECIST.

Exclusion Criteria:

Patients who

1. Are unable to swallow tablets.

2. Unable to discontinue use of carbamazepine, phenobarbital, and phenytoin.

3. Have previously been treated with an epidermal growth factor receptor (EGFR)
inhibitor, including erlotinib.

4. Are receiving concurrent administration of any other antitumor therapy.

5. Have received treatment within the last 30 days with a drug (not including study
drug) that has not received regulatory approval for any indication at the time of
study entry.