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Methotrexate capsules
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), Breast cancer, Lung cancer.
At a glance
| Generic name | Methotrexate capsules |
|---|---|
| Sponsor | Centocor, Inc. |
| Drug class | Antimetabolite; Folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology; Immunology |
| Phase | Phase 3 |
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)
- Breast cancer
- Lung cancer
- Rheumatoid arthritis
- Psoriasis
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Alopecia
- Infection
Key clinical trials
- A Study of Gefitinib, Trametinib, Disulfiram, and Sunitinib in Addition to Standard Chemotherapy in People With Osteosarcoma (PHASE2)
- Graft Versus Host Disease-Reduction Strategies for Donor Blood Stem Cell Transplant Patients With Acute Leukemia or Myelodysplastic Syndrome (MDS) (PHASE2)
- Study of Revumenib, Azacitidine, and Venetoclax in Pediatric and Young Adult Patients With Refractory or Relapsed Acute Myeloid Leukemia (PHASE1)
- Pembrolizumab + Chemotherapy in Newly Diagnosed PCNSL (PHASE1)
- Bruton's Tyrosine Kinase (BTK) Inhibitor, Ibrutinib, in Patients With Newly Diagnosed or Refractory/Recurrent Primary Central Nervous System Lymphoma (PCNSL) and Refractory/Recurrent Secondary Central Nervous System Lymphoma (SCNSL) (PHASE1, PHASE2)
- Combination of Methotrexate and Phototherapy Versus Phototherapy in Adults With Progressive Vitiligo (PHASE2)
- Methotrexate in Erosive Inflammatory Hand Osteoarthritis (PHASE4)
- Dose-Ranging Phase 2b Study of ABX464 in Moderate to Severe Ulcerative Colitis (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 |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |