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Tofacitinib with methotrexate
Tofacitinib with methotrexate is a JAK inhibitor + DMARD Small molecule drug developed by Pfizer. It is currently FDA-approved for Rheumatoid arthritis (moderate to severe, active), Polyarticular course juvenile idiopathic arthritis.
Tofacitinib inhibits Janus kinase (JAK) enzymes to suppress inflammatory cytokine signaling, while methotrexate provides additional immunosuppression through antifolate activity.
Tofacitinib, also known as CP-690,550, is being studied in combination with methotrexate for the treatment of Takayasu arteritis, a form of arthritis. This combination is being investigated in a randomized open-label study, NCT04299971, titled "Efficiency of Methotrexate and Tofacitinib in Mild and Moderate Patients" at Shanghai Zhongshan Hospital.
At a glance
| Generic name | Tofacitinib with methotrexate |
|---|---|
| Sponsor | Pfizer |
| Drug class | JAK inhibitor + DMARD |
| Target | JAK1, JAK3 (tofacitinib); dihydrofolate reductase (methotrexate) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tofacitinib is a JAK inhibitor that blocks JAK1 and JAK3 preferentially, disrupting the intracellular signaling of multiple inflammatory cytokines (IL-6, IL-23, IFN-γ, and others). Methotrexate acts as a disease-modifying antirheumatic drug (DMARD) by inhibiting dihydrofolate reductase and reducing cell proliferation. The combination provides synergistic immunosuppression for treating rheumatoid arthritis and other inflammatory conditions.
Approved indications
- Rheumatoid arthritis (moderate to severe, active)
- Polyarticular course juvenile idiopathic arthritis
Common side effects
- Upper respiratory tract infection
- Diarrhea
- Nausea
- Headache
- Elevated liver enzymes (ALT/AST)
- Hypertension
- Serious infections
- Lipid elevation
Key clinical trials
- Efficacy of Tofacitinib on Skin Thickening in Diffuse Cutaneous Systemic Sclerosis: A Comparative Study With Methotrexate (PHASE4)
- Tofacitinib vs Methotrexate for Severe Alopecia Areata (TOFA-MTX-AA) (PHASE4)
- Determination of the Optimal Treatment Target in Ulcerative Colitis (PHASE4)
- Methotrexate Combined With Tofacitinib in Rheumatoid Arthritis (NA)
- Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty (PHASE2)
- Induction and Tapering Therapy With Tofacitinib and Glucocorticoid in Patients With Polymyalgia Rheumatica (PHASE3)
- Treatment of Rheumatoid Arthritis With DMARDs: Predictors of Response (PHASE3)
- Efficacy of Tofacitinib, Methotrexate Combination Therapy Versus Upadacitinib, Methotrexate Combination Therapy in 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:
- Tofacitinib with methotrexate CI brief — competitive landscape report
- Tofacitinib with methotrexate updates RSS · CI watch RSS
- Pfizer portfolio CI
Frequently asked questions about Tofacitinib with methotrexate
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Related
- Drug class: All JAK inhibitor + DMARD drugs
- Target: All drugs targeting JAK1, JAK3 (tofacitinib); dihydrofolate reductase (methotrexate)
- Manufacturer: Pfizer — full pipeline
- Therapeutic area: All drugs in Immunology
- Indication: Drugs for Rheumatoid arthritis (moderate to severe, active)
- Indication: Drugs for Polyarticular course juvenile idiopathic arthritis
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing