Abstract: This study was to investigate the inhibitory effects of artemether in combination with etoposide on the proliferation and invasion ability of human small cell lung cancer cell line H446. H446 cells were treated with different concentrations of artemether or etoposide alone or their combination. The inhibitory effects on proliferation were detected by MTT assay, while cell cycle and apoptosis of H446 cells in each group were analyzed by flow cytometry using PI and Annexin V/PI-staining, respectively. The invasion capability of H446 cells in different groups was tested with matrigel-coated transwell. The results implicated that artemether or etoposide or their combination does inhibit proliferation of H446 cells dose-dependently. Artemether alone had little effect on the apoptosis of H446 cells while its combination with etoposide resulted in significantly apoptosis of H446 cells comparing with other groups(P< 0. 05). Etoposide blocked H446 progression markedly by arresting cell cycle in G₂ phase with percentage of cells in G₁ phase decreasing significantly while artemether alone or in combination with etoposide had little synergetic effect on cell cycle. Artemether or etoposite alone or their combination could dramatically inhibit the invasion ability of H446 cells.