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

Inclusion Criteria

• Diagnosis of non-small cell lung cancer.
• Prior treatment with a checkpoint inhibitor (as appropriate per cohort)
• Adequate bone marrow and organ function

Exclusion Criteria

• Uncontrolled tumor in the brain
• Unacceptable toxicity with prior checkpoint inhibitor
• Impaired heart function

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.

Trial Phase Phase II

Trial Type Treatment

Lead Organization
Mirati Therapeutics

• Primary ID MRTX-500
• Secondary IDs NCI-2016-01892
• Clinicaltrials.gov ID NCT02954991