GDC-0068 is a novel, highly selective oral ATP-competitive inhibitor designed to bind to the 3 isoforms of Akt. GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. GDC-0068 inhibits the growth and proliferation of cancer cell lines and xenograft models, including those with loss of PTEN function, oncogenic mutations in PIK3CA, and amplification of HER2. Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.