A Study of BGB324 in Combination With Erlotinib in Patients With Non-Small Cell Lung Cancer

This is a multi-center, multi-arm open-label Phase I/2 study that will be conducted at up to
4 clinical sites in the US.

Up to approximately 66 patients with histologically- or cytologically-confirmed Stage IIIb
or Stage IV non-small cell lung cancer will receive BGB324 as a single agent (Run-in Cohort)
or in combination with erlotinib (Arms A-C).

The dose of erlotinib will be 150 mg daily (Arms A - C). A dose of 100 mg daily will be
permitted in Arms B and C only. In Arm A, the dose of BGB324 will be escalated in a standard
3+3 fashion until an MTD of the combination is established. At this point, Arm B and Arm C
will be initiated. It is intended that the BGB324 MTD dose observed in Arm A will be used in
Arms B and C, but a lower dose level may be incorporated upon recommendation of the Safety
Review Committee. Dose escalation beyond the Arm A MTD level is not planned for Arm B or Arm
C.

Inclusion Criteria:

- Provision of written informed consent to participate in this investigational study

- Histological or cytological confirmation of Stage IIIb or Stage IV (unresectable)
NSCLC

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

- Age 18 years or older

- Known EGFR mutation status

- Has been receiving full dose erlotinib for treatment of NSCLC for at least six weeks
with erlotinib-related toxicities being well-controlled and less than Grade 3 in
severity at screening and is scheduled to continue treatment with erlotinib

- Female patients of childbearing potential must have a negative serum pregnancy test
within 7 days prior to taking their first dose of BGB324. Male patients and female
patients of reproductive potential must agree to practice highly effective methods of
contraception (such as hormonal implants, combined oral contraceptives, injectable
contraceptives, intrauterine device with hormone spirals, total sexual abstinence,
vasectomy) throughout the study and for ≥3 months after the last dose of BGB324.
Female patients are considered NOT of childbearing potential if they have a history
of surgical sterility, including tubal ligation, or evidence of post-menopausal
status defined as any of the following:

- Natural menopause with last menses >1 year ago

- Radiation induced oophorectomy with last menses >1 year ago

- Chemotherapy induced menopause with last menses >1 year ago

Exclusion Criteria:

- Pregnant or lactating

- Abnormal left ventricular ejection fraction (less than the lower limit of normal for
a patient of that age at the treating institution or <45%)

- Treatment with any of the following: histamine receptor two inhibitors, protocol pump
inhibitors or antacids within three days or five half-lives, whichever is longer

- History of an ischemic cardiac event including myocardial infarction within 3 months
of study entry

- NSCLC with evidence of a centrally cavitating lesion

- Pulmonary hemorrhage or hemoptysis > 2.5 mL blood within six weeks unless cause has
been addressed and is medically resolved

- Treatment with cytotoxic chemotherapy within the preceding four weeks

- Treatment with other non-cytotoxic agents for NSCLC in the preceding ten days or four
terminal half-lives, whichever is shorter

- Congestive cardiac failure of >Grade 2 severity according to the NYHA defined as
symptomatic at less than ordinary levels of activity

- Unstable cardiac disease, including unstable angina or unstable hypertension, as
defined by the need for change in medication for lack of disease control within the
last three months