RT Book, Section A1 Chabner, Bruce A. A2 Chabner, Bruce A. A2 Longo, Dan L. SR Print(0) ID 1127646297 T1 Antifolates T2 Harrison's Manual of Oncology, 2e YR 2016 FD 2016 PB McGraw-Hill Education PP New York, NY SN 9780071793254 LK hemonc.mhmedical.com/content.aspx?aid=1127646297 RD 2024/04/20 AB The antifolates were introduced as antileukemic drugs in 1948; in landmark experiments treating children with acute lymphocytic leukemia (ALL), Sidney Farber produced the first evidence that chemotherapy with a folate analogue, aminopterin, could lead to complete remissions (1). Methotrexate subsequently became the standard antifolate in treatment of ALL. It has since gained an important role in regimens for lymphomas, and choriocarcinoma, and as an immunosuppressive following allogeneic bone marrow transplantation. It is also a standard agent for treating rheumatoid arthritis, Wegener's granulomatosis, and other inflammatory/autoimmune diseases. Pemetrexed (Alimta), a closely related structure but with a different site of action, is widely used for non-small cell lung cancer, mesothelioma, and ovarian cancer. Pralatrexate, the newest antifolate similar in action to methotrexate, is highly active against peripheral T-cell lymphoma and cutaneous T-cell lymphoma.