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Methotrexate tablets
Methotrexate inhibits dihydrofolate reductase, blocking the synthesis of purines and pyrimidines required for DNA replication and cell division.
Methotrexate inhibits dihydrofolate reductase, blocking the synthesis of purines and pyrimidines required for DNA replication and cell division. Used for Acute lymphoblastic leukemia (ALL), Osteosarcoma, Breast cancer.
At a glance
| Generic name | Methotrexate tablets |
|---|---|
| Also known as | MTX, methotrexate pills |
| Sponsor | Yancheng First People's Hospital |
| Drug class | Antimetabolite / Folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology, Immunology, Rheumatology |
| Phase | FDA-approved |
Mechanism of action
By inhibiting dihydrofolate reductase, methotrexate prevents the conversion of dihydrofolate to tetrahydrofolate, disrupting one-carbon transfer reactions essential for nucleotide synthesis. This leads to suppression of rapidly dividing cells, including cancer cells and activated immune cells. At lower doses, it also has immunosuppressive and anti-inflammatory effects through adenosine release and other mechanisms.
Approved indications
- Acute lymphoblastic leukemia (ALL)
- Osteosarcoma
- Breast cancer
- Lung cancer
- Rheumatoid arthritis
- Psoriasis
- Crohn's disease
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis / stomatitis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Neurotoxicity (at high doses)
- Alopecia
- Infection
Key clinical trials
- Study on the Efficacy and Safety of the TmBU Conditioning Regimen in High-risk or Relapsed/Refractory Acute Leukemia (PHASE2)
- Phase 2 Study of Alisertib Therapy for Rhabdoid Tumors (PHASE2)
- Premedication to Reduce Amivantamab Associated Infusion Related Reactions (PHASE2)
- Venetoclax Basket Trial for High Risk Hematologic Malignancies (PHASE1)
- Study of Revumenib, Azacitidine, and Venetoclax in Pediatric and Young Adult Patients With Refractory or Relapsed Acute Myeloid Leukemia (PHASE1)
- A Trial to Examine the Interaction of Repinatrabit With Ethinyl Estradiol/Norethindrone, Metformin,Carbamazepine, Rosuvastatin, and Methotrexate When Administered Together (PHASE1)
- Molecular and Clinical Risk-Directed Therapy for Infants and Young Children With Newly Diagnosed Medulloblastoma (PHASE2)
- Methotrexate Alone vs Methotrexate + Etanercept for Minimal/Low Disease Activity in Juvenile Idiopathic Arthritis (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 |