Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer

Glesatinib is an orally administered multi-targeted tyrosine kinase inhibitor (TKI) that
primarily targets the Axl and Mesenchymal-Epithelial Transition (MET) receptors. Sitravatinib
is an orally-available, potent small molecule inhibitor of a closely related spectrum of
receptor tyrosine kinases (RTKs) including MET, Axl, MERTK, VEGFR family, PDGFR family, KIT,
FLT3, Trk family, RET, DDR2 and selected Eph family members. Mocetinostat is an orally
administered histone deacetylase (HDAC) inhibitor. Nivolumab is a human IgG monoclonal
antibody that binds to the programmed cell death-1(PD-1) receptor and blocks its interaction
with programmed cell death ligand-1 (PD-L1) and PD-L2, releasing PD-1 pathway-mediated
inhibition of the immune response including anti-tumor immune response. Combining an
immunotherapeutic PD-L1 checkpoint inhibitor with an agent that has both immune modulatory
and antitumor properties could enhance the antitumor efficacy observed with either agent
alone.

The study will begin with a lead-in dose escalation evaluation of two dose levels of each
investigational agent in combination with nivolumab. Following completion of the lead-in dose
escalation, enrollment into the Phase 2 study will proceed.

Inclusion Criteria:

- Diagnosis of non-small cell lung cancer.

- Prior treatment with platinum based doublet and checkpoint inhibitor

- Adequate bone marrow and organ function

Exclusion Criteria:

- Uncontrolled tumor in the brain

- Unacceptable toxicity with prior checkpoint inhibitor

- Impaired heart function