It is reported that overactivation of PIK3CA gene mutations affecting the PI3Kα catalytic subunit, such as H1047R, P449T, E545K and R88Q, are detected in about 15–20% of CRC, which makes PI3K pathway a potential attractive target [9, 10, 25, 26]. The gene discussed is PIK3CA; the disease is colorectal carcinoma.