Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis. This inhibition leads to suppression of inflammation as well as prevention of cell division. Because of these effects, methotrexate is often used to treat inflammation caused by arthritis or to control cell division in neoplastic diseases such as breast cancer and non-Hodgkin's lymphoma.
Due to the toxic effects of methotrexate, it is indicated for treatment of some forms of arthritis and severe psoriasis only if first line treatment has failed or patients are intolerant of those treatments.
Methotrexate was granted FDA approval on 7 December 1953.
Methotrexate oral solution is indicated for pediatric acute lymphoblastic leukemia and pediatric polyarticular juvenile idiopathic arthritis. Methotrexate injections for subcutaneous use are indicated for severe active rheumatoid arthritis, polyarticular juvenile idiopathic arthritis and severe, recalcitrant, disabling psoriasis.
Other formulations are indicated to treat gestational choriocarcinoma, chorioadenoma destruens, hydatiform mole, breast cancer, epidermoid cancer of the head and neck, advanced mycosis fungoides, lung cancer, and advanced non-Hodgkin's lymphoma. It is also used in the maintenance of acute lymphocytic leukemia. Methotrexate is also given before treatment with leucovorin to prolong relapse-free survival following surgical removal of a tumour in non-metastatic osteosarcoma.
Dr. Zvi Klein, Kefar-saba, Israel
Fred Hutch/University of Washington Cancer Consortium, Seattle, Washington, United States
Harbin Medical University Cancer Hospital, Harbin, China
Beijing Chao-Yang Hospital, Beijing, China
Cancer Hospital of Chinese Academy of Medical Science, Beijing, China
Investigational Site Number 392002, Sendai-Shi, Japan
Investigational Site Number 392001, Sendai-Shi, Japan
Aravind Eye Hospital, Pondicherry, Tamil Nadu, India
King Khaled Eye Specialist Hospital, Riyadh, Saudi Arabia
Royal Victorian Eye and Ear Hospital, Melbourne, Victoria, Australia
San Raffaele Scientific Institute, Milano, Italy
University of Cagliari, Cagliari, Italy
University of Milano-Bicocca San Gerardo Hospital, Monza, Italy
University of Pennsylvania, Philadelphia, Pennsylvania, United States
Greenville Hospital System University Medical Center, Greenville, South Carolina, United States
Univ of Calif., Los Angeles; Rheumatology, Los Angeles, California, United States
Cedars-Sinai Medical Center, Los Angeles, California, United States
Rheumatology Assoc. of S. Florida - Clinical Research Center, Boca Raton, Florida, United States
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