Currently, only a few chemotherapeutic agents (ifosfamide, mitomycin, vinblastine, and vindesine) have consistently produced single-agent response rates greater than 15% in patients with non-small-cell lung cancer (NSCLC). While combination chemotherapy with these and other agents may prolong survival in some patients with advanced disease, complete responses and long-term disease control are achieved only infrequently. In recent years, several new drugs have produced single-agent response rates above 20% in phase I/II trials. These results have brightened the prospects for chemotherapy against NSCLC. This article reviews available data for several of these agents: navelbine, which is an analogue of vinblastine, the camptothecins CTP-11 and topotecan, and taxol, the first of a novel class of antimicrotubule drugs.