3039 Background: AEE788 is an oral inhibitor with potent activity against multiple tyrosine kinases including EGFR, HER2, and VEGFR2. This phase 1 study was to assess the safety, pharmacokinetics (PK), pharmacodynamics (PD), MTD/DLT dose levels, and optimal biologic dose of AEE788. Methods: Patients (pts) with advanced solid tumors were enrolled. Doses were escalated in a standard Phase I design with 3–6 pts/cohort. Safety monitoring included extensive cardiac assessments. All but 1 pt were naive to EGFR and VEGF inhibitory therapy. Pharmacodynamic markers were analyzed in pre- and post-treatment skin and tumor biopsies. A 24-hr PK profile was obtained on days 1, 15, and 28, with trough sampling on days 8 and 22. Each cycle (cyc) is 28 days. Results: To date, 69 pts, median age 55 years (range 20–78), have been treated with once daily AEE788 at doses of 25 (5), 50 (6), 100 (5), 150 (5), 225 (6), 300 (8), 400 (14), 450 (5), 500 (6), and 550 mg (9) per day. Tumor types treated were breast (10), colon (9), m...