Phase 1b Trial of BGJ398/BYL719 in Solid Tumors

This dose escalation/dose expansion study will evaluate the combination of orally
administered BGJ398 in combination with orally administered BYL719. During the dose
escalation part, the MTD of the combination will be determined in patients whose advanced or
metastatic tumors express mutations to PIK3CA. Once the MTD has been determined, the
expansion part will begin. Patients will be addd to one of three arms based on the disease
type and genetic changes. Patients with metastatic colorectal cancer are not eligible for
participation in the expansion part.

Inclusion Criteria:

- Histologically/cytologically confirmed advanced or metastatic solid tumors who have
failed standard therapy or for whom no effective standard anti-cancer therapy exists

- Documented PIK3CA mutations in all patients in dose escalation and expansion with or
without documented genetic alterations in FGFR depending upon dose expansion cohort
(either local or central determination)

- Measurable disease defined by RECIST v1.1

- ECOG performance status of ≤2

Exclusion Criteria:

- Prior PI3Ki or selective FGFR inhibitor treatment (for patients enrolled to expansion
part)

- Colorectal cancer (for patients enrolled to expansion part)

- Patients with diabetes mellitus requiring insulin treatment and/or with clinical
signs or with fasting glucose ≥ 140 mg/dL / 7.8 mmol/L, history of clinically
significant gestational diabetes mellitus or documented steroid-induced diabetes
mellitus

- Use of medications that increase serum levels of phosphorus and/or calcium

- Inorganic phosphorus outside of normal limits

- Total and ionized serum calcium outside of normal limits