Abstract

Antifolates, which are inhibitors of the folate biosynthetic pathway, have been shown to be effective in inhibiting the growth of proliferating malignant mammalian cells as well as proliferating bacterial and protozoal infections. Drugs that target the folate pathway have a substantial impact on cancer therapy. The development of new antifolate-based anticancer drugs with improved features and activities is still a common approach in medicinal and pharmaceutical research. Antifolates are a subject of great and significant interest worldwide. Despite decades of research in antifolates, there are few compounds that are therapeutically used throughout all indications, such as methotrexate, pralatrexate, Tomudex, and pemetrexed. The antifolate drugs are classified into classical and nonclassical antifolates, and they remain an important tool to guide the design of novel antifolates. The most commonly used FDA-approved drugs were discussed in this chapter.

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