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Methotrexate (low dose)
Methotrexate is a folate antagonist that inhibits dihydrofolate reductase, blocking DNA synthesis and cell division in rapidly proliferating cells.
Methotrexate is a folate antagonist that inhibits dihydrofolate reductase, blocking DNA synthesis and cell division in rapidly proliferating cells. Used for Various malignancies (specific indication context-dependent on Case Comprehensive Cancer Center trial), Autoimmune and inflammatory conditions (at low dose).
At a glance
| Generic name | Methotrexate (low dose) |
|---|---|
| Also known as | amethopterin, Folex, methylaminopterin, Mexate, MTX |
| Sponsor | Case Comprehensive Cancer Center |
| Drug class | Antimetabolite; folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology; Immunology |
| Phase | Phase 3 |
Mechanism of action
Methotrexate competitively inhibits dihydrofolate reductase, an enzyme essential for converting dihydrofolate to tetrahydrofolate, which is required for one-carbon transfer reactions in nucleotide synthesis. This disruption of DNA and RNA synthesis preferentially affects rapidly dividing cells, including cancer cells and activated immune cells. At low doses, methotrexate also has immunosuppressive and anti-inflammatory effects through adenosine release and other mechanisms.
Approved indications
- Various malignancies (specific indication context-dependent on Case Comprehensive Cancer Center trial)
- Autoimmune and inflammatory conditions (at low dose)
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Alopecia
- Infection
Key clinical trials
- Venlafaxine as Adjunct Therapy in Rheumatoid Arthritis (PHASE2)
- Chemotherapy With Targeted-Immunotherapy for Newly Diagnosed Ph+ ALL (NA)
- Full-Course Immunotherapy Consolidation for Unfit or Fit B-ALL Who Decline Chemotherapy (PHASE2)
- Study on the Efficacy and Safety of the TmBU Conditioning Regimen in High-risk or Relapsed/Refractory Acute Leukemia (PHASE2)
- LBL-2016 for Children or Adolescents in China (PHASE3)
- A Multicenter Two-Cohort Study of Methotrexate, Rituximab, Sintilimab and Pirtobrutinib for Treatment-Naive PCNSL vs. Real-World Investigator-Selected Treatment (Observational Cohort) (PHASE2)
- CApivasertib, Venetoclax And Low-intensity chemotheRapY for Adults With ALL/LBL (PHASE1, PHASE2)
- A Study to Compare Standard Chemotherapy to Therapy With CPX-351 and/or Gilteritinib for Patients With Newly Diagnosed AML With or Without FLT3 Mutations (PHASE3)
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 |
|---|---|
| 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 (low dose) CI brief — competitive landscape report
- Methotrexate (low dose) updates RSS · CI watch RSS
- Case Comprehensive Cancer Center portfolio CI