Phase 1 Dose Escalation Study of CGX1321 in Subjects With Advanced Gastrointestinal Tumors

Inclusion Criteria:

• Histologically-diagnosed advanced Gl tumors, such as colorectal adenocarcinoma,gastric adenocarcinoma, pancreatic adenocarcinoma, bile duct carcinoma, hepatocellularcarcinoma, esophageal carcinoma that have relapsed or are refractory to or are notconsidered medically suitable to receive standard of care treatment

• Eastern Cooperative Oncology Group (ECOG) score of 0 - 1

• Minimum estimated life expectancy of 3 months

• Adequate organ function

• Recovery from prior treatment-related toxicities

• Ability to swallow capsules

• Willingness for subjects of reproductive potential to use adequate methods ofcontraception during and for 3 months after study treatment

Exclusion Criteria:

• Prior exposure to a WNT inhibitor

• Received previous therapy for malignancy within 21 days

• Major surgery within 4 weeks of first dose of study drug

• Radiotherapy within 2 weeks of first dose of study drug

• Significant GI or variceal bleeding or subdural hematoma within 3 months of treatmentstart

• Uncontrolled central nervous system metastases or leptomeningeal metastases

• Requirement for immunosuppressive agents (must be off for at least 7 days)

• Currently receiving medications that are known CYP3A4/5 inhibitors. Patients currentlyreceiving medications of known inducers of CYP3A4/5 or substrates of CYP2C8/9 andCYP1A2 may be excluded.

• Bone abnormalities

• Hypercalcemia

• Cardiac abnormalities

• Known human immunodeficiency virus positive, or active hepatitis A, B or C

• History of additional prior malignancy with the exception of surgically curedcarcinomas such as skin, prostate, bladder, thyroid, cervix or other carcinomas insitu

• Active systemic infection requiring intravenous antibiotics within 2 weeks oftreatment start

• Pregnancy or lactation