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Methotrexate Monotherapy
Methotrexate inhibits dihydrofolate reductase, blocking folate metabolism and reducing DNA synthesis and cell proliferation.
Methotrexate inhibits dihydrofolate reductase, blocking folate metabolism and reducing DNA synthesis and cell proliferation. Used for Acute lymphoblastic leukemia (ALL), Osteosarcoma, Breast cancer.
At a glance
| Generic name | Methotrexate Monotherapy |
|---|---|
| Sponsor | Bangladesh Medical University |
| Drug class | Antimetabolite / Folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology, Immunology, Rheumatology |
| Phase | FDA-approved |
Mechanism of action
Methotrexate is a folate antagonist that inhibits the enzyme dihydrofolate reductase, preventing the conversion of dihydrofolate to tetrahydrofolate, which is essential for one-carbon transfer reactions in nucleotide synthesis. This leads to decreased DNA and RNA synthesis, resulting in reduced cell proliferation. At lower doses used in autoimmune conditions, it also has immunosuppressive and anti-inflammatory effects through adenosine release and other mechanisms.
Approved indications
- Acute lymphoblastic leukemia (ALL)
- Osteosarcoma
- Breast cancer
- Rheumatoid arthritis
- Psoriasis
- Crohn's disease
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis / stomatitis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Alopecia
- Infection
- Diarrhea
Key clinical trials
- A Phase 3 Study to Evaluate Petosemtamab Compared With Investigator's Choice Monotherapy in Previously Treated Head and Neck Squamous Cell Carcinoma Patients (PHASE3)
- Lorlatinib for Newly-Diagnosed High-Grade Glioma With ROS or ALK Fusion (EARLY_PHASE1)
- Comparative Study of Leflunomide Plus Methotrexate Versus Methotrexate Monotherapy in Refractory Polyarticular Juvenile Idiopathic Arthritis Patients (PHASE4)
- Kinetics of Elimination of Methotrexate and Its Major Metabolite 7-OH-methotrexate for Observant Patients (NA)
- Eflornithine (DFMO) for Ewing Sarcoma and Osteosarcoma (PHASE2)
- Switching From Intravenous to Subcutaneous Infliximab in Adult Patients With Inflammatory Bowel Disease (NA)
- A Study of Revumenib in Combination With Chemotherapy for Patients Diagnosed With Relapsed or Refractory Leukemia (PHASE2)
- Methotrexate Treatment of Arthritis Caused by Chikungunya Virus (MARCH) (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 Monotherapy CI brief — competitive landscape report
- Methotrexate Monotherapy updates RSS · CI watch RSS
- Bangladesh Medical University portfolio CI