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.
Route: IV, PO, IM, IT, SC, intraarterial
Extravasation: inflammitant

• 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

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.

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
• Diffuse large B-cell lymphoma
• Extranodal NK/T-cell lymphoma, nasal type
• Head and neck cancer
• Hemophagocytic lymphohistiocytosis
• Histiocytoses
• HIV-associated lymphoma
• Large granular lymphocytic leukemia
• Mantle cell lymphoma
• NK/T-cell lymphoma
• Osteosarcoma
• Penile cancer
• Peripheral T-cell lymphoma
• Prostate cancer
• Small cell lung cancer
• T-cell acute lymphoblastic leukemia
• Transplant conditioning regimens

Patient drug information

• Methotrexate (Otrexup) subcutaneous injection package insert
• Methotrexate (MTX) patient drug information (Chemocare)
• Methotrexate (MTX) patient drug information (UpToDate)

History of changes in FDA indication

• 12/7/1953: Initial FDA approval

Also known as

Synonyms
Abitrexate	Alltrex	Amethopterin	Antifolan	APO-Methotrexate	Artrait	Biometrox	Biotrexate
Caditrex	Cytotrexate	Ebetrexat	Emthexat	Emthexate	Emthexate PF	Emthexate S	Ervemin
Farmitrexat	Fauldmetro	Folex PFS	Folitrax	Hextrate	Ifamet	Imutrex,Ledertrexate	Ledertrexate Sodium
Ledertrexato	Lumexon	Matrex	Maxtrex	Medsatrexate	Merex	Metex	Methobax
Methoblastin	Methorex	Methotrexaat	Methotrexaat Sandoz	Methotrexat Biosyn	Methotrexat Ebewe	Methotrexate Bigmar	Methotrexate Bristol
Methotrexate DBL	Methotrexate Disodium	Methotrexate DUP	Methotrexate Ebewe	Methotrexate Farmos	Methotrexate Knoll	Methotrexate Lederle	Methotrexate LPF
Methotrexate Mayne	Methotrexate Merck	Methotrexate Paranova	Methotrexate R	Methotrexate Remedica	Methotrexate Singad	Methotrexate Sodium	Methotrexate Sodium Lederle
Methotrexate Teva	Methotrexate Wyeth	Methotrexat Lederle	Methotrexat Medac	Methotrexato	Methotrexat Ridupharm	Methotrexat Teva	Methotrexatum
Meticil	Metolate	Metotressato	Metotrexate	Metotrexato Asofarma	Metotrexato Chiesi	Metotrexato Dosa	Metotrexato Filaxis
Metotrexato Lederle	Metotrexato Martian	Metotrexato Microsules	Metotrexol	Metrex	Metrexan	Metrexato	Metrotex
Mexate	Miantrex CS	MTX	MTX Hexal	Neometho	Neotrexate	Novatrex	Oncotrex
Oncotrex-PF	O Trexat	P&U Methotrexate	Pharmatrexate	Ratio-Methotrexate	Remtrex	Reumatrex	Rextop
Rheumatrex	Tecnomet	Texate	Texate T	Texorate	Tratoben	Trav Methotrexate	Tremetex
Trexall	Trexan	Trexeron	Trixilem	Trixilem RU	Unitrexate	Vero Methotrexate	Zexate