An Open Label Two-stage Study of Orally Administered BKM120 in Patients With Metastatic Non-small Cell Lung Cancer With Activated PI3K Pathway

Inclusion Criteria:

- Histologically confirmed NSCLC with activated PI3K pathway

- Progressive disease after prior systemic antineoplastic treatment(s) for advanced
NSCLC

- Archival or fresh tumor biopsy must be available for profiling

- Measurable and/or non-measurable disease as per RECIST 1.1 criteria

- Eastern Cooperative Oncology Group (ECOG) performance status ≤ 2

- Adequate organ function as assessed by laboratory tests

Exclusion Criteria:

- Patient has received previous treatment with PI3K inhibitors

- Patient with squamous NSCLC has received more than one line of chemotherapy
treatment for metastatic disease; patient with non-squamous NSCLC has received more
than two lines of systemic antineoplastic treatment for metastatic disease

- Uncontrolled or symptomatic CNS metastases

- Concurrent use of any other approved or investigational antineoplastic agent

- Radiotherapy ≤ 28 days prior to starting study drug

- Major surgery within 28 days prior to starting study drug

- History of clinically significant cardiac dysfunction, mood disorders, or poorly
controlled diabetes mellitus

- Current treatment with medication that has a known risk to prolong the QT interval or
inducing Torsades de Pointes

- Impairment of gastrointestinal (GI) function

- Chronic treatment with steroids or another immunosuppressive agent.

- Concurrent severe and/or uncontrolled medical condition

- Currently receiving Warfarin or another coumarin derivative

- Known history of HIV infection

- Sensory neuropathy with functional impairment (CTC grade 2 neuropathy, regardless of
causality)

- Pregnancy, lactation, or breastfeeding

- Woman of child-bearing potential

Other protocol-defined inclusion/exclusion criteria may apply