Angiogenesis is an essential component of tumor growth and metastasis. To date, an anti-VEGF antibody, bevacizumab, in combination with paclitaxel and carboplatin in the first-line setting is the only approved antiangiogenic treatment in non-small-cell lung cancer (NSCLC). Angiokinase inhibitors are oral small-molecule agents. They not only inhibit the VEGF pathway, but also target other important signaling pathways contributing to angiogenesis: the PDGF and FGF pathways. Several angiokinase inhibitors have been studied or are in investigations for the treatment of NSCLC, and we review the current developmental status and future perspectives of these inhibitors (including sorafenib, sunitinib, motesanib and nintedanib) in NSCLC.