Methotrexate is an antineoplastic agent used the treatment of a wide variety of cancers as well as severe psoriasis, severe rheumatoid arthritis, and juvenile rheumatoid arthritis. Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis.
- Mechanism
- Curator reviewed · 4 references
Methotrexate enters tissues and is converted to a methotrexate polyglutamate by folylpolyglutamate.
Methotrexate's mechanism of action is due to its inhibition of enzymes responsible for nucleotide synthesis including dihydrofolate reductase, thymidylate synthase, aminoimidazole caboxamide ribonucleotide transformylase (AICART), and amido phosphoribosyltransferase. Inhibtion of nucleotide synthesis prevents cell division.
In rheumatoid arthritis, methotrexate polyglutamates inhibit AICART more than methotrexate. This inhibition leads to accumulation of AICART ribonucleotide, which inhibits adenosine deaminase, leading to an accumulation of adenosine triphosphate and adenosine in the extracellular space, stimulating adenosine receptors, leading to anti-inflammatory action.
- Primary indication
- Methotrexate oral solution is indicated for pediatric acute lymphoblastic leukemia and pediatric polyarticular juvenile idiopathic arthritis.Curator reviewed · 32 structured indications
- Formula / weight
- C20H22N8O5 · 454.4393 g/mol (avg)
- First approval
- Canada, 2003 · United States, 1953 · European Union, 2016
- Also known as
- Alpha-Methopterin · Amethopterin · methylaminopterin
- Code names
- ADX-2191 · CL-14377 · EMT-25299 · NSC-740 · R-9985 · WR-19039
- Brand names
Resolves to
FBOZXECLQNJBKD-ZDUSSCGKSA-NSMILESCN(CC1=CN=C2N=C(N)N=C(N)C2=N1)C1=CC=C(C=C1)C(=O)N[C@@H](CCC(O)=O)C(O)=OWhat you can answer from here — as of September 13, 2026
Which drugs share a target with Methotrexate, and which of those have an active Phase 3 trial?
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