Tofacitinib
XELJANZ
Pronunciation: toe-fa-SYE-ti-nib
“Zelly J, the Toffee City nibbler”
jack → Janus kinase (JAK) inhibitor
What it isJAK inhibitor; rheumatoid and psoriatic arthritis, ulcerative colitis, and ankylosing spondylitis.
Why this oneOral option after TNF-inhibitor failure; with methotrexate, as effective as adalimumab.
What limits itSerious infection, malignancy, cardiovascular events, thrombosis, and mortality warnings drive patient selection.
Pearls
- Breastfeeding: wait 18 h after IR, 36 h after XR dose.
- Dose can often be reduced in sustained remission.
Tofacitinib prescription history
Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Tofacitinib enters in 2012 (estimated).
FDA-approved for
- rheumatoid arthritis (2012)
- psoriatic arthritis, ulcerative colitis, ankylosing spondylitis
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| RA, PsA, or AS | Adult | 5 mg BID | 5 mg BID | |
| PsA or pcJIA | Peds >=2 yr, >=10 kg | 5 mg BID (>=40 kg) or weight-based (<40 kg) | ||
| Ulcerative colitis - induction | Adult | 10 mg BID x8 wk (max 16 wk) | 10 mg BID | |
| Ulcerative colitis - maintenance | Adult | 5 mg BID | 5 mg BID | 10 mg BID (shortest duration) |
Renal Reduce dose in moderate or severe renal impairment (CLcr <=50 mL/min)
Hepatic Reduce dose in moderate impairment; not recommended in severe
Instructions
- Do not initiate if ALC <500, ANC <1,000/mm3, or Hgb <9 g/dL.
- XELJANZ XR is not substitutable with immediate-release tofacitinib.
- Screen for TB and viral hepatitis before initiation.
Available strengths
- tab 5, 10 mg
- sol 1 mg/mL
- ER tab 11, 22 mg
Cautions
- Serious infections (bacterial, fungal, viral, TB, opportunistic)
- Increased mortality vs TNF blockers (RA >=50 yr with CV risk factor)
- Malignancies incl. lymphoma and NMSC
- Major adverse cardiovascular events
- Thrombosis (DVT, PE, arterial)
- GI perforation; lymphopenia, neutropenia, anemia, lipid elevations
Adverse reactions
- Upper respiratory tract infection
- Nasopharyngitis
- Diarrhea
- Headache
- (UC) elevated cholesterol
Pregnancy Insufficient human data to assess risk
Lactation Present in human milk (published data)
Cost
Generic entry2026
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Self-check
- Which kinase family does tofacitinib inhibit?
JAK. - Which comparator was used in the safety comparison that changed tofacitinib’s role?
A TNF blocker.