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Pronunciation | /ˌmɛθəˈtrɛkˌseɪt, ˌmiː-, -θoʊ-/ [1][2][3] |
Trade names | Trexall, Rheumatrex, Otrexup, others[4] |
Other names | MTX, amethopterin |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682019 |
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Routes of administration | By mouth, intravenous, intramuscular, subcutaneous, intrathecal |
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Bioavailability | 60% at lower doses, less at higher doses.[7] |
Protein binding | 35–50% (parent drug),[7] 91–93% (7-hydroxymethotrexate)[8] |
Metabolism | Hepatic and intracellular[7] |
Elimination half-life | 3–10 hours (lower doses), 8–15 hours (higher doses)[7] |
Excretion | Urine (80–100%), feces (small amounts)[7][8] |
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ECHA InfoCard | 100.000.376 |
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Formula | C20H22N8O5 |
Molar mass | 454.447 g·mol−1 |
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Methotrexate, formerly known as amethopterin, is a chemotherapy agent and immune-system suppressant.[4] It is used to treat cancer, autoimmune diseases, and ectopic pregnancies.[4] Types of cancers it is used for include breast cancer, leukemia, lung cancer, lymphoma, gestational trophoblastic disease, and osteosarcoma.[4] Types of autoimmune diseases it is used for include psoriasis, rheumatoid arthritis, and Crohn's disease.[4] It can be given by mouth or by injection.[4]
Common side effects include nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth.[4] Other side effects may include liver disease, lung disease, lymphoma, and severe skin rashes.[4] People on long-term treatment should be regularly checked for side effects.[4] It is not safe during breastfeeding.[4] In those with kidney problems, lower doses may be needed.[4] It acts by blocking the body's use of folic acid.[4]
Methotrexate was first made in 1947 and initially was used to treat cancer, as it was less toxic than the then-current treatments.[9] In 1956 it provided the first cures of a metastatic cancer.[10] It is on the World Health Organization's List of Essential Medicines.[11][12] Methotrexate is available as a generic medication.[4] In 2021, it was the 132nd most commonly prescribed medication in the United States, with more than 4 million prescriptions.[13][14]