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 used
- Acute promyelocytic leukemia
- Adult T-cell leukemia-lymphoma
- B-cell acute lymphoblastic leukemia
- Bladder cancer
- Breast cancer
- Burkitt lymphoma
- CNS leukemia
- CNS lymphoma
- Cutaneous T-cell lymphoma
- Diffuse large B-cell lymphoma
- Extranodal NK/T-cell lymphoma, nasal type
- Gestational trophoblastic neoplasia
- Head and neck cancer
- Hemophagocytic lymphohistiocytosis
- HIV-associated lymphoma
- Langerhans cell histiocytosis
- Large granular lymphocytic leukemia
- Mantle cell lymphoma
- Medulloblastoma
- NK/T-cell lymphoma
- Osteosarcoma
- Penile cancer
- Peripheral T-cell lymphoma
- Prostate cancer
- Small cell lung cancer
- T-cell acute lymphoblastic leukemia
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
- 12/7/1953: Initial FDA approval
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 | 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 |
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 chemotherapy
- Antimetabolites
- Antifolates
- Immunosuppressants
- 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
- Diffuse large B-cell lymphoma medications
- Extranodal NK/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/T-cell lymphoma medications
- Osteosarcoma medications
- Penile cancer medications
- Peripheral T-cell lymphoma medications
- Prostate cancer medications
- Small cell lung cancer medications
- T-cell acute lymphoblastic leukemia medications
- FDA approved in 1953
- WHO Essential Cancer Medicine