Lung cancer is one of the most prevalent cancers in the world. A cisplatin-based chemotherapy regimen is commonly used to major patients who have adenocarcinoma. Because of the limited remission rate, many patients need receive second-line treatment after receiving first-line chemotherapy. Drug screenings carried out currently are mainly from single phase. In consideration of systemic treatment, evaluation of a novel drug candidate from the point of view of first-line and second-line treatment is supposed to be important in the process of drug screening. In this review, we propose a flow of searching for new drugs, which is tailored to accommodate to first-line and second-line treatment in clinic.