ABSTRACT

Introduction .............................................................................................................. 82 Biology of the PI3K Pathway .................................................................................. 82 PI3K-AKT-mTOR Pathway in Cancer ...................................................................87 Agents Targeting PI3K-AKT-mTOR Pathway ....................................................... 91

PI3K Inhibitors .................................................................................................... 91 BKM120 (NVP-BKM120; Novartis) ............................................................. 91 XL147 (SAR245408; Exelixis and Sanofi-Aventis) .......................................95 GDC-0941 (Genentech) .................................................................................95 PX-866 (Oncothyreon) ...................................................................................96 CAL-101 (Calistoga Pharmaceuticals) ...........................................................96