A Study of Mutant Selective-Inhibitor (CGT6297), in Patients With Advanced Solid Tumors

Prior treatment

• Received small molecule chemotherapy or anticancer therapies or radiotherapy within certain timeframes before first dose of study drug.
• Major surgeries (eg, abdominal laparotomy) within 4 weeks of the first dose of study drug
• Treatment with radiotherapy ≤2 weeks before the first dose of study drug.
• Ongoing or planned long-term (≥4 consecutive weeks) treatment with glucocorticoid steroids at greater than physiologic dosing (defined as equivalent to \>20 mg/day prednisone)

Other illness

• Clinically significant cardiac disease

Lab values

• Diagnosis of diabetes mellitus type 1 or uncontrolled diabetes mellitus type 2 (defined as fasting glucose ≥140 mg/dL and HbA1c ≥7.0%; antihyperglycemic medical management permitted with the exception of insulin)
• Previous molecular testing (NGS or PCR) showed tumor with the following mutations: mutations/deletions in PTEN or activating mutations in AKT, HRAS/KRAS/NRAS, EGFR, and BRAF

• Histologically confirmed advanced solid tumor harboring oncogenic PIK3CA mutations in blood and/or tumor:
  • Phase 1b Cohort 1, participants must have PIK3CA endometrial cancer
  • Phase 1b Cohort 2, participants must have HR-positive/HER2-negative or HER2-low breast cancer (immunohistochemistry \[IHC\] and in-situ hybridization results must meet ASCO-College of American Pathology guidelines for breast cancer or criteria)
  • Phase 1b Cohort 3 will allow all solid tumors that do not meet criteria for Phase 1b Cohorts 1 or 2, including head and neck cancers, other gynecological cancers, colorectal cancers harboring PIK3CA mutations
• Meet prior treatment requirement of:
  • Phase 1a: previously treated with and refractory to or intolerant of existing therapy(ies) known to provide clinical benefit for their condition.
  • Phase 1b: previously treated with or considered not appropriate for SOC first-line treatment for their condition
• Have at least one measurable lesion according to RECIST v1.1.
• Eastern Cooperative Oncology Group (ECOG) Performance Status 0 to 1
• Have clinically acceptable local laboratory screening results (clinical chemistry and hematology) within certain limits
• Resolution of acute toxicities from prior anticancer therapy to ≤Grade 1 (or baseline), including resolution of clinically significant laboratory abnormalities (other than parameters specified in screening testing as outlined below), as determined by the National Cancer Institute-Common Terminology Criteria for Adverse Events (NCICTCAE) v5.0.
• Have an ejection fraction ≥50%