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Placebo to Methotrexate
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 Rheumatoid arthritis, Various malignancies (acute leukemia, lymphoma, breast cancer), Psoriasis.
At a glance
| Generic name | Placebo to Methotrexate |
|---|---|
| Sponsor | Amgen |
| Drug class | Antimetabolite / Folate antagonist |
| Target | Dihydrofolate reductase (DHFR) |
| Modality | Small molecule |
| Therapeutic area | Oncology / Immunology / Rheumatology |
| Phase | Phase 3 |
Mechanism of action
Methotrexate is a folate antagonist that inhibits dihydrofolate reductase, an enzyme critical for converting dihydrofolate to tetrahydrofolate, which is essential for one-carbon transfer reactions in nucleotide synthesis. By depleting intracellular folate cofactors, it suppresses DNA and RNA synthesis, leading to reduced cell proliferation and increased apoptosis. At lower doses used in rheumatologic conditions, it also has immunomodulatory effects including reduced T-cell activation and cytokine production.
Approved indications
- Rheumatoid arthritis
- Various malignancies (acute leukemia, lymphoma, breast cancer)
- Psoriasis
- Inflammatory bowel disease
Common side effects
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Mucositis / stomatitis
- Nausea and vomiting
- Hepatotoxicity
- Nephrotoxicity
- Alopecia
- Infection
Key clinical trials
- A Study to Investigate the Clinical Effect and the Safety of PRX-115 Infused Intravenously at Different Dosing Regimens, With and Without Methotrexate, Versus Placebo in Adults Gout Patients (RELEASE) (PHASE2)
- A Clinical Study of Tulisokibart (MK-7240) to Treat Rheumatoid Arthritis (RA) (MK-7240-014) (PHASE2)
- Extended vs Short-term Abatacept Dosing for Graft Versus Host Disease Prophylaxis (PHASE2)
- A Study to Assess the Safety and Efficacy of Different Doses of ELV001 to Treat Active Rheumatoid Arthritis in Patients With an Inadequate Response to Methotrexate and Tumor Necrosis Factor Inhibition (START SYNERGY) (PHASE2)
- A Study to Evaluate the Safety, Tolerability, and Drug Levels of BMS-986454 in Participants With Rheumatoid Arthritis (PHASE1)
- CD40L Antagonism in Rheumatoid Arthritis (RA) (PHASE2)
- Combination of Methotrexate and Phototherapy Versus Phototherapy in Adults With Progressive Vitiligo (PHASE2)
- Study to Assess Change in Disease Activity and Adverse Events of Oral Upadacitinib Compared to Subcutaneous Adalimumab in Adult Participants With Moderate to Severe Rheumatoid 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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Placebo to Methotrexate CI brief — competitive landscape report
- Placebo to Methotrexate updates RSS · CI watch RSS
- Amgen portfolio CI