XELJANZ
XELJANZ (tofacitinib citrate) is a Janus kinase (JAK) inhibitor indicated for the treatment of several chronic inflammatory conditions in patients who have had an inadequate response or intolerance to one or more TNF blockers. The medication is approved for use in adults with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and ulcerative colitis, as well as pediatric patients with psoriatic arthritis and polyarticular course juvenile idiopathic arthritis. It is available in multiple formulations, including tablets, extended-release tablets, and an oral solution. Use of the drug in combination with biologic therapies or potent immunosuppressants such as azathioprine and cyclosporine is not recommended.
How XELJANZ Works
Tofacitinib is an inhibitor of Janus kinase (JAK) enzymes, which are intracellular components that transmit signals from cytokine or growth factor receptors on the cell membrane. By inhibiting these enzymes, the drug prevents the phosphorylation and activation of Signal Transducers and Activators of Transcription (STATs) that modulate gene expression. This action interferes with signaling pathways involved in immune cell function and hematopoiesis. Tofacitinib specifically inhibits the activities of various JAK combinations, including JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2.
Details
- Status
- Prescription
- First Approved
- 2012-11-06
- Routes
- ORAL
- Dosage Forms
- TABLET, SOLUTION
XELJANZ Approval History
What XELJANZ Treats
5 indicationsXELJANZ is approved for 5 conditions since its original approval in 2012. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Moderately to severely active rheumatoid arthritis
- Active psoriatic arthritis
- Active ankylosing spondylitis
- Moderately to severely active ulcerative colitis
- Active polyarticular course juvenile idiopathic arthritis
XELJANZ Boxed Warning
SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), leading to hospitalization or death. Interrupt XELJANZ/XELJANZ XR treatment if serious infection occurs until the infection is ...
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), leading to hospitalization or death. Interrupt XELJANZ/XELJANZ XR treatment if serious infection occurs until the infection is controlled. Test for latent TB before and during therapy; treat latent TB prior to use. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test. ( 5.1 ) • Higher rate of all-cause mortality, including sudden cardiovascular (CV) death with XELJANZ vs. TNF blockers in rheumatoid arthritis (RA) patients. ( 5.2 ) • Malignancies have occurred in patients treated with XELJANZ. Higher rate of lymphomas and lung cancers with XELJANZ vs. TNF blockers in RA patients. ( 5.3 ) • Higher rate of major adverse CV events (defined as CV death, myocardial infarction, and stroke) with XELJANZ vs. TNF blockers in RA patients. ( 5.4 ) • Thrombosis has occurred in patients treated with XELJANZ. Increased incidence of pulmonary embolism, venous and arterial thrombosis with XELJANZ vs. TNF blockers in RA patients. ( 5.5 ) SERIOUS INFECTIONS Patients treated with XELJANZ (tablets and oral solution) or XELJANZ XR (extended-release tablets) are at increased risk for developing serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), that may lead to hospitalization or death [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids. Reported infections included: • Active TB, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent TB bef
XELJANZ Target & Pathway
ProTarget
A member of the JAK family involved in signaling for interferons and several interleukins. JAK1 inhibition is effective in rheumatoid arthritis, atopic dermatitis, and other inflammatory conditions by blocking multiple cytokine pathways.
XELJANZ Competitors
Pro10 other drugs also target JAK1. Compare mechanisms, indications, and trial activity.
Competitors share the same molecular target (JAK1). Earlier expiry dates signal biosimilar/generic opportunities.
Drugs Similar to XELJANZ
FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
XELJANZ FDA Label Details
ProIndications & Usage
FDA Label (PDF)XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets) are Janus kinase (JAK) inhibitors. XELJANZ tablets and XELJANZ XR are indicated for the treatment of adult patients with: • Moderately to severely active rheumatoid arthritis (RA), who have had an inadequate response or intolerance to one or more TNF blockers. • Active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers. • Active ankylosing spondylitis (AS), who have had an inadequate response or intolerance to one or more TNF blockers. • Moderately to severely ac...
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bac...
XELJANZ Patents & Exclusivity
Patents (10 active)
Exclusivity
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.