The novel agent pemetrexed inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase. Significant activity has been seen in completed phase II trials of pemetrexed in non-small cell lung cancer and breast cancer. Pemetrexed is also active in combination with other agents such as gemcitabine, cisplatin, and carboplatin. In addition, this agent shows promising activity in bladder, head and neck, esophageal, renal, and cervical carcinomas. Preliminary results of studies in these tumor types are reviewed.
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