Methotrexate (MTX)
General information
Class/mechanism: Folate analog, antimetabolite, interferes with DNA synthesis. Methotrexate inhibits dihydrofolic acid reductase, which catalyzes reactions that produce tetrahydrofolates, which are used in purine nucleotide and thymidylate synthesis.[1][2][3][4][5][6][7]
Route: IV, PO, IM, IT, SC, intraarterial
Extravasation: inflammitant
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Toxicity
Monitoring of plasma levels
- Stoller RG, Hande KR, Jacobs SA, Rosenberg SA, Chabner BA. Use of plasma pharmacokinetics to predict and prevent methotrexate toxicity. N Engl J Med. 1977 Sep 22;297(12):630-4. link to original article PubMed
Reversal agents
- Glucarpidase (Voraxaze) can be used to treat toxic plasma methotrexate concentrations (greater than 1 micromole per liter) in patients with delayed methotrexate clearance due to impaired renal function
Diseases for which it is established (work in progress)
Diseases for which it is used
- Acute myeloid leukemia
- Acute promyelocytic leukemia
- B-cell acute lymphoblastic leukemia
- Bladder cancer
- Breast cancer
- CNS leukemia
- Desmoid tumors
- Gestational trophoblastic neoplasia
- Head and neck cancer
- Hemophagocytic lymphohistiocytosis
- Langerhans cell histiocytosis
- Large granular lymphocytic leukemia
- Medulloblastoma
- Non-Hodgkin lymphoma
- Penile cancer
- Testicular cancer
- T-cell acute lymphoblastic leukemia
Diseases for which it was used
- Colon cancer
- Follicular lymphoma
- Gastric cancer
- Hodgkin lymphoma
- Non-small cell lung cancer
- Ovarian cancer
- Prostate cancer
- Small cell lung cancer
Patient drug information
- Methotrexate (Otrexup) subcutaneous injection package insert[5]
- Methotrexate (MTX) patient drug information (Chemocare)[8]
- Methotrexate (MTX) patient drug information (UpToDate)[9]
History of changes in FDA indication
- 1953-12-07: Initial FDA approval
- Uncertain date: Methotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole. (No supporting studies are cited)
- Uncertain date: In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. (No supporting studies are cited)
- Uncertain date: Methotrexate is also indicated in the treatment of meningeal leukemia. (No supporting studies are cited)
- Uncertain date: Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. (No supporting studies are cited)
- Uncertain date: Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas. (No supporting studies are cited)
- Uncertain date: Methotrexate in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non- metastatic osteosarcoma who have undergone surgical resection or amputation for the primary tumor. (No supporting studies are cited)
Also known as
- Generic names: amethopterin, MTX
- Brand names:
Synonyms | |||||||
---|---|---|---|---|---|---|---|
Abitrexate | Alltrex | Antifolan | Artrait | Biometrox | Biotrexate | Caditrex | Cytotrexate |
Ebetrexat | Emthexat | Emthexate | Ervemin | Farmitrexat | Fauldmetro | Folex PFS | Folitrax |
Hextrate | Ifamet | Imutrex | Jylamvo | Ledertrexate | Ledertrexato | Lumexon | Matrex |
Maxtrex | Medsatrexate | Merex | Metex | Methobax | Methoblastin | Methorex | Methotrexaat |
Methotrexat | Methotrexato | Methotrexatum | Meticil | Metolate | Metotressato | Metotrexate | Metotrexato |
Metotrexol | Metrex | Metrexan | Metrexato | Metrotex | Mexate | Miantrex CS | Neometho |
Neotrexate | Nordimet | Novatrex | Oncotrex | O Trexat | Pharmatrexate | Remtrex | Reumatrex |
Rextop | Rheumatrex | Tecnomet | Texate | Texorate | Tratoben | Tremetex | Trexall |
Trexan | Trexeron | Trixilem | Unitrexate | Zexate |
References
- ↑ 1.0 1.1 Methotrexate (MTX) tablet package insert
- ↑ Methotrexate (MTX) tablet package insert (locally hosted backup)
- ↑ Methotrexate (MTX) injection package insert
- ↑ Methotrexate (MTX) injection package insert (locally hosted backup)
- ↑ 5.0 5.1 Methotrexate (Otrexup) subcutaneous injection package insert
- ↑ Methotrexate (Otrexup) subcutaneous injection package insert (locally hosted backup)
- ↑ Otrexup manufacturer's website
- ↑ Methotrexate (MTX) patient drug information (Chemocare)
- ↑ Methotrexate (MTX) patient drug information (UpToDate)
- Drugs
- Intramuscular medications
- Intrathecal medications
- Intravenous medications
- Oral medications
- Subcutaneous medications
- Inflammitant
- Antimetabolites
- Antifolates
- Immunosuppressants
- Acute myeloid leukemia medications
- Acute promyelocytic leukemia medications
- Adult T-cell leukemia-lymphoma medications
- B-cell acute lymphoblastic leukemia medications
- Bladder cancer medications
- Breast cancer medications
- Burkitt lymphoma medications
- CNS lymphoma medications
- CNS leukemia medications
- Cutaneous T-cell lymphoma medications
- Desmoid tumor medications
- Diffuse large B-cell lymphoma medications
- Extranodal NK- and T-cell lymphoma, nasal type medications
- Gestational trophoblastic neoplasia medications
- Head and neck cancer medications
- Hemophagocytic lymphohistiocytosis medications
- HIV-associated lymphoma medications
- Langerhans cell histiocytosis medications
- Large granular lymphocytic leukemia medications
- Mantle cell lymphoma medications
- Medulloblastoma medications
- NK- and T-cell lymphoma medications
- Osteosarcoma medications
- Penile cancer medications
- Peripheral T-cell lymphoma medications
- Testicular cancer medications
- T-cell acute lymphoblastic leukemia medications
- Colon cancer medications (historic)
- Follicular lymphoma medications (historic)
- Gastric cancer medications (historic)
- Classical Hodgkin lymphoma medications (historic)
- Non-small cell lung cancer medications (historic)
- Ovarian cancer medications (historic)
- Prostate cancer medications (historic)
- Small cell lung cancer medications (historic)
- FDA approved in 1953
- WHO Essential Cancer Medicine