Pemetrexed is an antifolate chemotherapy drug used to treat cancers like non-small cell lung cancer and malignant pleural mesothelioma. It works by inhibiting multiple enzymes involved in folate metabolism, disrupting DNA and RNA synthesis, and preventing cancer cell growth. Developed in the 1990s by Eli Lilly, it was approved by the FDA in 2004 and is often combined with cisplatin to improve effectiveness, marking a significant advancement in multi-targeted cancer therapy.