Key

Inclusion Criteria:

1. Adult patients (≥ 18 years)

2. Histologically or cytologically-documented NSCLC (EGFR mutation status must be known)

3. Brain metastases from NSCLC, which:

have radiologically-progressed after WBRT or are present without prior WBRT

4. At least one radiologically-confirmed and measurable lesion (≥ 1.0 cm in the longest
diameter) within14 days prior to the first dose of GRN1005 (Cycle 1, Day 1), as
follows: an intra-cranial disease lesion (≥ 1.0 cm in the longest diameter) confirmed
by Gd-MRI, or an extra-cranial disease lesion (≥ 1.0 cm in the longest diameter)
confirmed by MRI or CT scan with contrast Prior stereotactic radiosurgery (SRS) is
allowed; however, metastatic brain lesions previously treated with SRS are not
allowed as target or as non-target lesions.

5. Patients must be neurologically stable, defined as being on stable doses of
corticosteroids and anticonvulsants (not EIAEDs, including phenytoin, phenobarbitol,
carbamazepine, fosphenytoin, primidone, oxcarbazepine) for ≥ 5 days prior to
obtaining the baseline Gd-MRI of the brain and ≥ 5 days prior to first dose of
GRN1005 (Cycle 1, Day 1).

6. Karnofsky Performance Score (KPS) ≥ 80%

7. Completed WBRT for intra-cranial lesions ≥ 28 days prior to first dose of GRN1005
(with the exception of local radiation therapy for palliation to extra-cranial sites,
i.e., bone). All clinically significant toxicities must have resolved to ≤ NCI CTCAE
v4.0 Grade 1.0.

Key Exclusion Criteria:

1. NCI CTCAE v4.0 Grade ≥ 2 neuropathy

2. CNS disease requiring immediate neurosurgical intervention (e.g., resection, shunt
placement, etc.)

3. Known intra-cranial hemorrhage

4. Known leptomeningeal disease