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METHOTREXATE
METHOTREXATE is a drug. It is currently FDA-approved (first approved 1953).
Methotrexate is a small molecule used in the treatment of conditions such as rheumatoid arthritis and upper tract urothelial carcinoma. It has been studied in various clinical trials, including those involving chemotherapy protocols like M-VAC and combinations with other drugs like gemcitabine and cisplatin.
At a glance
| Generic name | METHOTREXATE |
|---|---|
| Modality | Small molecule |
| Phase | FDA-approved |
| First approval | 1953 |
Approved indications
Boxed warnings
- WARNING: EMBRYO-FETAL TOXICITY, HYPERSENSITIVITY REACTIONS, and SEVERE ADVERSE REACTIONS • Methotrexate tablets can cause embryo-fetal toxicity, including fetal death. For non-neoplastic diseases, methotrexate tablets are contraindicated in pregnancy. For neoplastic diseases, advise females and males of reproductive potential to use effective contraception [see Contraindications (4), Warnings and Precautions (5.1), Use in Specific Populations (8.1, 8.3)]. • Methotrexate tablets are contraindicated in patients with a history of severe hypersensitivity reactions to methotrexate, including anaphylaxis [Contraindications (4), Warnings and Precautions (5.2)]. • Serious adverse reactions, including death, have been reported with methotrexate. Closely monitor for adverse reactions of the bone marrow, gastrointestinal tract, liver, lungs, skin, and kidneys. Withhold or discontinue methotrexate tablets as appropriate [Warnings and Precautions (5.3, 5.4, 5.5, 5.6, 5.7, 5.8)]. WARNING: EMBRYO-FETAL TOXICITY, HYPERSENSITIVITY REACTIONS, and SEVERE ADVERSE REACTIONS See full prescribing information for complete boxed warning. • Methotrexate tablets can cause embryo-fetal toxicity, including fetal death. For non-neoplastic diseases, Methotrexate tablets are contraindicated in pregnancy. For neoplastic diseases, advise patients of reproductive potential of the potential risk to a fetus and to use effective contraception. (4, 5.1, 8.1, 8.3) • Methotrexate tablets are contraindicated in patients with a history of severe hypersensitivity reactions to methotrexate, including anaphylaxis. (4, 5.2) • Serious adverse reactions, including death, have been reported with methotrexate. Closely monitor for adverse reactions of the bone marrow, gastrointestinal tract, liver, lungs, skin, and kidneys. Withhold or discontinue methotrexate tablets as appropriate. (5.3, 5.4, 5.5, 5.6, 5.7, 5.8)
Common side effects
- Elevated liver function tests
- Nausea/Vomiting
- Stomatitis
- Thrombocytopenia
- Rash/Pruritis/Dermatitis
- Diarrhea
- Alopecia
- Leukopenia
- Pancytopenia
- Dizziness
- Gastrointestinal reactions
- Headache
Key clinical trials
- Testing the Addition of the Anti-cancer Drug Venetoclax and/or the Anti-cancer Immunotherapy Blinatumomab to the Usual Chemotherapy Treatment for Infants With Newly Diagnosed KMT2A-rearranged or KMT2A-non-rearranged Leukemia (PHASE2)
- A Study to Investigate Blinatumomab in Combination With Chemotherapy in Patients With Newly Diagnosed B-Lymphoblastic Leukemia (PHASE3)
- Pediatric-Inspired Regimen Combined With Venetoclax and Immunotherapy for Adult Ph-Negative Acute Lymphoblastic Leukemia (NA)
- A Study to Test the Addition of the Drug Cabozantinib to Chemotherapy in Patients With Newly Diagnosed Osteosarcoma (PHASE2, PHASE3)
- Testing the Addition of MEDI4736 (Durvalumab) to Chemotherapy Before Surgery for Patients With High-Grade Upper Urinary Tract Cancer (PHASE2, PHASE3)
- Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia (PHASE2)
- Testing the Use of Steroids and Tyrosine Kinase Inhibitors With Blinatumomab or Chemotherapy for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia in Adults (PHASE3)
- Venlafaxine as Adjunct Therapy in Rheumatoid Arthritis (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- METHOTREXATE CI brief — competitive landscape report
- METHOTREXATE updates RSS · CI watch RSS
Frequently asked questions about METHOTREXATE
What is METHOTREXATE?
METHOTREXATE is a Small molecule drug.
When was METHOTREXATE approved?
METHOTREXATE was first approved on 1953.
What development phase is METHOTREXATE in?
METHOTREXATE is FDA-approved (marketed).
What are the side effects of METHOTREXATE?
Common side effects of METHOTREXATE include Elevated liver function tests, Nausea/Vomiting, Stomatitis, Thrombocytopenia, Rash/Pruritis/Dermatitis, Diarrhea.
Related
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing