XELJANZ XR (tofacitinib citrate)
XELJANZ XR is indicated for the treatment of Rheumatoid Arthritis; Psoriatic Arthritis; Ankylosing Spondylitis; Ulcerative Colitis; Polyarticular Juvenile Idiopathic Arthritis.
How XELJANZ XR Works
Tofacitinib is a Janus kinase (JAK) inhibitor that targets the intracellular signaling pathways of cytokines and growth factors involved in hematopoiesis and immune cell function. It works by inhibiting JAK enzymes (primarily JAK1, JAK2, and JAK3), which prevents the phosphorylation and activation of Signal Transducers and Activators of Transcription (STATs). By disrupting this JAK-STAT signaling pathway, tofacitinib modulates gene expression and reduces the pro-inflammatory cellular response.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2016-02-23
- Patent Cliff
- 2034
- Routes
- ORAL
- Dosage Forms
- TABLET, EXTENDED RELEASE
XELJANZ XR Approval History
What XELJANZ XR Treats
5 indicationsXELJANZ XR is approved for 5 conditions since its original approval in 2016. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Rheumatoid Arthritis
- Psoriatic Arthritis
- Ankylosing Spondylitis
- Ulcerative Colitis
- Polyarticular Juvenile Idiopathic Arthritis
XELJANZ XR 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 XR 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 XR Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in XELJANZ XR's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications XELJANZ XR treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to XELJANZ XR
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
2 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT05487963 | CGB-500-001 | Ph 1, Ph 2 | completed | Tolerability and Effectiveness of CGB-500 Topical Ointment, 1% Tofacitinib, for the Treatment of Atopic Dermatitis |
| NCT04468425 | AC-1101-PK-001 | Ph 1 | completed | Tofacitinib Citrate Topical Gel 3.2% FDA BA Bridging Study |
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 XR FDA Label Details
Indications & Usage
FDA Label (PDF)XELJANZ XR is indicated for the treatment of Rheumatoid Arthritis; Psoriatic Arthritis; Ankylosing Spondylitis; Ulcerative Colitis; Polyarticular Juvenile Idiopathic Arthritis.
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 XR Patents & Exclusivity
Patents (8 active)
Pro Intelligence Preview
Deep insights for XELJANZ XR
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2034
- • 36 active patents
Trial Analysis
- • 65 total trials
- • Stage: Expansion
Competitive Landscape
- • 20 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Related Intelligence
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment