Phase 1/1b Study to Evaluate the Safety and Tolerability of CPI-444 Alone and in Combination With Atezolizumab in Advanced Cancers

This is a phase 1/1b open-label, multicenter, dose-selection study of CPI-444, an oral small
molecule targeting the adenosine-A2A receptor on T-lymphocytes and other cells of the immune
system. This trial will study the safety, tolerability, and anti-tumor activity of CPI-444 as
a single agent and in combination with atezolizumab, an intravenous PD-L1 inhibitor. CPI-444
blocks adenosine from binding to the A2A receptor. Adenosine suppresses the anti-tumor
activity of T cells and other immune cells.

Inclusion Criteria

1. Eastern Cooperative Oncology Group (ECOG) Performance Status 0-1.

2. Documented incurable cancer with one of the following histologies: non-small cell lung
cancer, malignant melanoma, renal cell cancer, triple negative breast cancer,
colorectal cancer with microsatellite instability (MSI), bladder cancer, and
metastatic castration resistant prostate cancer.

3. At least 1 measurable lesion per Response Evaluation Criteria in Solid Tumors (RECIST
1.1).

4. At least 1 but not more than 5 prior systemic therapies for advanced/recurrent or
progressing disease.

Exclusion Criteria

1. History of severe hypersensitivity reaction to monoclonal antibodies.

2. Any active autoimmune disease or a documented history of serious autoimmune disease
within the past 5 years requiring immunosuppressive therapy.

3. History of idiopathic pulmonary fibrosis, organizing pneumonia, drug-induced
pneumonitis, idiopathic pneumonitis, or clinical symptoms of active pneumonitis.

4. The use of any investigational medication or device in the 30 days prior to screening
and throughout the study is prohibited.

5. If a patient is currently receiving denosumab, this must be discontinued prior to
enrollment. Substitution with biphosphonates are acceptable.