ALIMTA is a novel, multi-targeted antifolate which inhibits several enzymes of the folate pathways and it has demonstrated a broad spectrum of clinical activity in multiple tumor types, including colorectal, breast, non-small cell lung cancer (NSCLC), pancreatic, head and neck, bladder and cervical cancers. ALIMTA has been tested in different patient populations, including those who have received no prior chemotherapy, those who have relapsed following prior platinum-containing therapy, and those who have relapsed following prior chemotherapy without platinum. In every group was demonstrated an activity comparable to currently used new drugs. ALIMTA was also studied in association with cisplatin in chemotherapy-naive patients and the overall response rate is comparable to other current combination regimens. From December 1999, an amendment has been made to all studies to add vitamin supplementation to reduce toxicity and early indications are that the frequency of serious toxicities resulting from ALIMTA treatment has been reduced. On the basis of the results of the studies reviewed, it is clear that ALIMTA is emerging as a new drug in the management of NSCLC.