Advanced non–small cell lung cancer (NSCLC) has long been a diagnosis with few treatment options and poor outcomes. However, recent discoveries about the molecular biology of NSCLC are changing the way it is treated. Driver mutations that cause uncontrolled cancer cell proliferation have been discovered in some types of NSCLC. This has led to the discovery of therapies that can target a specific driver mutation in advanced NSCLC and halt cancer progression. This article reviews standard treatment of NSCLC and explores the targetable mutations of NSCLC, available targeted treatments, treatment obstacles, and the future of targeted therapy in NSCLC.