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Pemetrexed is a small molecule chemotherapy drug classified as an antifolate antineoplastic agent. It is primarily used to treat malignant pleural mesothelioma and non-squamous non-small cell lung cancer (NSCLC), either alone or in combination with other agents such as cisplatin or pembrolizumab[1][2][3]. Pemetrexed works by inhibiting several folate-dependent enzymes essential for DNA and purine synthesis—specifically thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT)[3][6][8]. This inhibition disrupts DNA replication and repair in rapidly dividing cancer cells. The drug is administered intravenously, typically every 21 days, and patients often receive supplemental folic acid, vitamin B12, and corticosteroids to reduce side effects[2][5]. Pemetrexed was developed by Eli Lilly and Company.
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