Xeljanz (Xeljanz XR)

Pronunciation: toe-fa-SIT-i-nib.

Generic name
tofacitinib (as citrate)
Drug class
Janus kinase (JAK) inhibitor
Form
Immediate-release tablet (5 mg, 10 mg); extended-release tablet (11 mg, 22 mg); oral solution (1 mg/mL)
Route
Oral
Legal status
Prescription-only

Supply Rules Vary

Trade names by country: United States · United Kingdom · Canada · Australia · New Zealand

Australia: XELJANZ XR (5), XELJANZ (5) · Full directory

What tofacitinib (as citrate) is and how it works

Xeljanz (tofacitinib) is an oral Janus kinase (JAK) inhibitor approved to treat several inflammatory conditions: rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis (all adults), and polyarticular course juvenile idiopathic arthritis (children 2 years and older), each following an inadequate response to or intolerance of one or more TNF blockers. (1)

Tofacitinib carries a real, current FDA boxed warning -- the FDA's strongest safety warning -- covering serious infections, an increased risk of death, cancer, serious heart-related events, and blood clots. This warning is based on a large clinical trial (called ORAL Surveillance) conducted specifically with tofacitinib in rheumatoid arthritis patients aged 50 and older who had at least one cardiovascular risk factor, comparing it to a different class of medicine (a TNF blocker). Because of these findings, the higher 10 mg twice-daily dose is not recommended for most of tofacitinib's approved uses and is reserved only for a limited period when treating ulcerative colitis. Your prescriber will discuss these risks with you, screen you for infections such as tuberculosis before starting treatment, and monitor you closely throughout.

Mechanism of action: how tofacitinib (as citrate) works

Tofacitinib is an oral small-molecule inhibitor of Janus kinases (JAK), predominantly JAK1 and JAK3, with functional selectivity over JAK2. Inhibition of JAK1 and JAK3 by tofacitinib attenuates signalling by multiple cytokines involved in the inflammatory and immune response, including interleukins and interferons. (1) (2)

What tofacitinib (as citrate) is used for

Rheumatoid arthritis

Treatment of moderately to severely active rheumatoid arthritis in adults who have had an inadequate response or intolerance to one or more TNF blockers. In the UK, used in combination with methotrexate. (1) (2)

Psoriatic arthritis

Treatment of active psoriatic arthritis in adults, and in pediatric patients 2 years and older (US), who have had an inadequate response or intolerance to one or more TNF blockers. (1) (2)

Ankylosing spondylitis

Treatment of active ankylosing spondylitis in adults who have had an inadequate response or intolerance to one or more TNF blockers. (1) (2)

Polyarticular course juvenile idiopathic arthritis (pcJIA)

Treatment of active polyarticular course juvenile idiopathic arthritis in pediatric patients 2 years and older who have had an inadequate response or intolerance to one or more TNF blockers. (1) (2)

Ulcerative colitis

Treatment of moderately to severely active ulcerative colitis in adults who have had an inadequate response or intolerance to one or more TNF blockers. This is the only indication for which the higher 10 mg twice-daily (or XR 22 mg once-daily) dose is used, and only for a time-limited induction period (typically 8 weeks, extendable to 16 weeks) before transitioning to a lower maintenance dose. In Australia, this is the ONLY indication for which the 10 mg dose is approved at all -- it is not approved there for rheumatoid arthritis or psoriatic arthritis. (1) (5)

Before taking tofacitinib (as citrate)

Do not take / not appropriate for

  • Do not take tofacitinib if you have had an allergic reaction to it or any of its ingredients. (all confirmed markets) (1) (2)
  • Do not take tofacitinib if you have active tuberculosis, sepsis, or another serious or opportunistic infection. This is an explicit contraindication in the UK; the current US label does not list a formal contraindication for this but treats active serious infection as a reason to avoid starting or to interrupt treatment. (United Kingdom (contraindication); United States (avoid/interrupt)) (2) (1)
  • Do not take tofacitinib if you have severe liver (hepatic) impairment -- an explicit contraindication in the UK; the US label similarly does not recommend use in severe hepatic impairment. (United Kingdom (contraindication); United States (not recommended)) (2) (1)
  • Do not take tofacitinib if you are pregnant or breastfeeding -- an explicit contraindication in the UK; the current US label advises against breastfeeding but does not list a formal pregnancy contraindication. (United Kingdom (contraindication); United States (lactation advisory)) (2) (1)

Tell your clinician about

  • Any history of tuberculosis (active or latent) or exposure to someone with TB -- you should be tested for latent TB before starting treatment.
  • Any history of recurrent or chronic infections, or shingles (herpes zoster).
  • Your age -- if you are 65 or older, this affects the real risk/benefit balance for tofacitinib, per specific regulator guidance in the EU and UK.
  • Whether you currently smoke or have smoked in the past -- this is a real, specific risk factor called out by regulators for cardiovascular events and malignancy.
  • Any personal or family history of heart disease, blood clots, stroke, or heart attack.
  • Any history of cancer.
  • Any history of stomach or intestinal problems, such as diverticulitis.
  • All other medicines you take, especially other immunosuppressants or CYP2C19/CYP3A4 inhibitors.
  • Kidney or liver problems.
  • Pregnancy, plans for pregnancy, or breastfeeding.
  • Any recent or planned vaccinations, especially live vaccines.
(1) (2) (3)

How to take tofacitinib (as citrate)

  • Take tofacitinib exactly as prescribed, with or without food.
  • XELJANZ XR (extended-release) tablets must be swallowed whole -- do not crush, split, or chew them.
  • XELJANZ XR is not interchangeable with XELJANZ tablets/oral solution; any switch between them should be made by your healthcare provider, not on your own.
  • Do not change your dose or stop taking tofacitinib without talking to your prescriber first.
  • Attend all follow-up appointments and blood tests so your prescriber can monitor for infection, blood count changes, liver enzyme changes, and lipid changes.
(1) (2)

Procedures and treatment changes

Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3) (4) (5) (6)

Missed dose

If you miss a dose, contact your prescriber or pharmacist for guidance on how to proceed, rather than following a self-directed rescheduling rule -- this is especially important given tofacitinib's dosing limitations and monitoring requirements.

Overdose

Seek urgent medical attention or contact a poison control centre if too much tofacitinib may have been taken, or if you develop signs of infection, unusual bleeding, chest pain, sudden shortness of breath, or leg swelling (possible signs of a blood clot). There is no specific antidote; management is supportive. (1)

Side effects

Side effects and their urgency vary; report severe, persistent, or concerning symptoms.

Upper respiratory tract infection, nasopharyngitis, headache -- common across indications.

What to notice: Upper respiratory tract infection, nasopharyngitis, headache -- common across indications.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Diarrhea, nausea -- common.

What to notice: Diarrhea, nausea -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Elevated cholesterol/lipid levels -- common, requires monitoring.

What to notice: Elevated cholesterol/lipid levels -- common, requires monitoring.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Hypertension, lymphopenia, anemia, rash -- common.

What to notice: Hypertension, lymphopenia, anemia, rash -- common.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Increased blood creatine phosphokinase, herpes zoster -- reported in >=5% of adult ulcerative colitis patients.

What to notice: Increased blood creatine phosphokinase, herpes zoster -- reported in >=5% of adult ulcerative colitis patients.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)

Serious warnings

Serious infections, including tuberculosis — boxed_warning

Symptoms: Fever, cough, night sweats, weight loss, or other signs of infection.

Action: You should be tested for latent tuberculosis before starting treatment and monitored during therapy, even if your initial TB test was negative. Contact your prescriber immediately if you develop signs of infection -- treatment is typically interrupted until the infection is controlled. (1) (2)

Increased risk of death (mortality) — boxed_warning

Symptoms: This is a population-level risk identified in a large clinical trial, not a specific symptom to watch for.

Action: A large clinical trial (ORAL Surveillance) in rheumatoid arthritis patients 50 years and older with a cardiovascular risk factor found a higher rate of all-cause mortality, including sudden cardiovascular death, with tofacitinib compared to a TNF blocker. This is why the higher 10 mg twice-daily dose is not recommended for most indications. Discuss your individual risk with your prescriber, especially if you are 65 or older or have cardiovascular risk factors. (1) (3)

Malignancy (cancer), including lymphoma and lung cancer — boxed_warning

Symptoms: Unexplained weight loss, persistent cough, unusual lumps or swelling, or other new or unusual symptoms.

Action: Malignancies, including lymphomas and solid tumors, have occurred in patients treated with tofacitinib. A higher rate of malignancies (excluding non-melanoma skin cancer) was observed compared to TNF blockers, with lymphomas and lung cancers observed at a higher rate; current or past smokers are at additional increased risk. Discuss your individual cancer risk factors with your prescriber. (1) (2)

Major adverse cardiovascular events (heart attack, stroke, cardiovascular death) — boxed_warning

Symptoms: Chest pain, shortness of breath, sudden weakness or numbness on one side of the body, difficulty speaking.

Action: Seek emergency medical attention immediately if these symptoms occur. Treatment should be discontinued if you experience a heart attack or stroke. Patients 50 and older with at least one cardiovascular risk factor had a higher rate of these events compared to a TNF blocker in a large clinical trial. (1) (2)

Blood clots (thrombosis), including pulmonary embolism and deep vein thrombosis — boxed_warning

Symptoms: Sudden shortness of breath, chest pain, rapid breathing, leg swelling, pain, or redness (often in the calf).

Action: Seek emergency medical attention immediately if these symptoms occur. Blood clots, some fatal, have occurred in patients treated with tofacitinib and other JAK inhibitors. Tell your prescriber if you are at increased risk for blood clots. (1) (2)

Gastrointestinal perforation — high caution

Symptoms: New-onset severe abdominal pain, especially with fever, chills, nausea, or vomiting.

Action: Tell your prescriber immediately or seek emergency care -- this is particularly important if you have a history of diverticulitis or take corticosteroids/NSAIDs. (1)

Low blood counts (lymphopenia, neutropenia, anemia) — moderate caution

Symptoms: Unusual tiredness, signs of infection, or unusual bleeding/bruising.

Action: Your prescriber will monitor your blood counts regularly and may interrupt or adjust treatment if levels fall too low. (1) (2)

Interactions

  • Potent CYP3A4 inhibitors (e.g. ketoconazole): significantly increase tofacitinib exposure -- dose reduction required. (2) (1)
  • Combined moderate CYP3A4 and potent CYP2C19 inhibitors (e.g. fluconazole): increase tofacitinib exposure -- dose reduction required. (2)
  • Potent CYP inducers (e.g. rifampicin): decrease tofacitinib exposure; concomitant use with potent inducers is not recommended. (2)
  • Methotrexate: no dose adjustment needed when combined with tofacitinib for rheumatoid arthritis. (2)
  • Live vaccines: avoid concurrent use with XELJANZ/XELJANZ XR given the immunosuppressive effect. (1)
  • Other biologic DMARDs or potent immunosuppressants (e.g. azathioprine, cyclosporine): combination use is not recommended given additive immunosuppression risk. (1)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy

Contraindicated in the UK; tofacitinib has shown teratogenic effects in rats and rabbits. Women of childbearing potential should use effective contraception during treatment and for at least 4 weeks after the final dose. The current US label does not list a formal pregnancy contraindication but pregnancy-related risk should be discussed directly with your prescriber. (1) (2) (3) (4) (5) (6)

Breastfeeding

Contraindicated in the UK -- risk to the breastfed child cannot be excluded. The current US label advises against breastfeeding while taking tofacitinib. (1) (2) (3) (4) (5) (6)

Children

Approved for psoriatic arthritis and polyarticular course juvenile idiopathic arthritis in children 2 years and older (weighing at least 10 kg), with weight-based dosing, in the US and UK. (1) (2) (3) (4) (5) (6)

Elderly

Patients 65 years of age and older are specifically named in the EU regulatory restriction: tofacitinib should be used in this group only if no suitable treatment alternative is available, given the increased risk of serious infections, myocardial infarction, malignancies, and all-cause mortality. (1) (2) (3) (4) (5) (6)

Smokers

Current or past smokers are specifically identified across multiple regulator sources as being at additional increased risk of cardiovascular events and malignancy with tofacitinib. (1) (2) (3) (4) (5) (6)

Hepatic_impairment

Not recommended in patients with severe hepatic impairment; an explicit contraindication in the UK. (1) (2) (3) (4) (5) (6)

Renal_impairment

Dose adjustment guidance provided in the full prescribing information for patients with moderate to severe renal impairment; consult the current full label. (1) (2) (3) (4) (5) (6)

Source_ids

US-DAILYMED-XELJANZ-2026,UK-EMC-XELJANZ-5MG-SMPC-2026,EU-EMA-XELJANZ-DHPC-PRAC-2021 (1) (2) (3) (4) (5) (6)

Monitoring

Before starting

  • Active and latent tuberculosis testing
  • Viral hepatitis screening
  • Complete blood count (avoid starting if lymphocyte count <500 cells/mm3, absolute neutrophil count <1000 cells/mm3, or hemoglobin <9 g/dL)
  • Baseline liver function evaluation
  • Update immunizations according to current guidelines before starting

During treatment

  • Regular monitoring for signs and symptoms of infection, including TB, even if the initial test was negative.
  • Periodic complete blood counts, liver enzymes, and lipid panel.
  • Monitoring for signs of malignancy, cardiovascular events, and blood clots.
  • Prompt evaluation of any new-onset severe abdominal pain (possible gastrointestinal perforation).
(1)

Storage

Store at room temperature, away from moisture and light, out of reach of children.

Professional information

Clinician-facing context only, sourced from the current US, UK, EU, Canadian, Australian, and New Zealand sources reviewed; verify against the current full label before prescribing, and note the market-specific dosing-limitation and contraindication differences described above.

United States

Indication: RA, PsA, AS (adults); pcJIA, PsA (pediatric 2+ years); UC (adults) -- all after inadequate response/intolerance to TNF blockers

Dose summary: 5 mg BID (or XR 11 mg once daily) for RA/PsA/AS/pcJIA; 10 mg BID (or XR 22 mg once daily) for UC induction only (8-16 weeks), then step down to 5 mg BID/XR 11 mg maintenance. 10mg/XR22mg NOT recommended for RA/PsA/AS/pcJIA. Contraindications: none listed.

Renal context: Dose modification required per the full label for renal impairment; consult current full prescribing information. (1)

United Kingdom / European Union

Indication: RA (with methotrexate), PsA, AS, UC (adults); pcJIA (pediatric 2+ years) -- subject to a specific 2021 PRAC restriction for patients 65+/smokers/CV-risk/malignancy-risk (use only if no suitable alternative)

Dose summary: Same core dose structure as the US (5mg BID standard, 10mg BID for UC induction only), with explicit contraindications: active TB/serious infection, severe hepatic impairment, pregnancy, and lactation.

Renal context: Dose reduction required with potent CYP3A4 inhibitors or combined CYP3A4/CYP2C19 inhibitors. (2) (3)

Canada, Australia, New Zealand

Indication: Canada: RA, PsA, AS, UC (Serious Warnings and Precautions box matching US/UK content). Australia: RA, PsA, AS -- 10mg dose approved ONLY for UC, excluded entirely from RA/PsA. New Zealand: RA (generic Tofacitinib Devatis), specialist-initiated only.

Dose summary: Core dosing follows the same 5mg/10mg BID structure, with Australia's stricter exclusion of the 10mg dose from RA/PsA specifically.

Renal context: Consult the current full local label for renal dose-adjustment guidance. (4) (5) (6)

Mechanism of action

Overdose note

No specific antidote. Manage supportively, with monitoring for infection, cytopenias, and cardiovascular/thrombotic events. (1) (2)

Frequently asked questions

Does Xeljanz (tofacitinib) carry a boxed warning?

Yes -- a real, current FDA boxed warning covering five components: serious infections (including tuberculosis), increased risk of death, cancer (malignancy), major adverse cardiovascular events (heart attack, stroke, cardiovascular death), and blood clots (thrombosis). This warning is based on a large clinical trial (ORAL Surveillance) conducted directly with tofacitinib in rheumatoid arthritis patients 50 and older with a cardiovascular risk factor, comparing it to a TNF blocker. (1)

Is the higher 10 mg dose of tofacitinib used for all conditions it treats?

No. The 10 mg twice-daily dose (or Xeljanz XR 22 mg once daily) is not recommended for rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, or polyarticular course juvenile idiopathic arthritis in the US or UK. It is used only for a time-limited induction period when treating ulcerative colitis, after which the dose is typically reduced. In Australia, the 10 mg dose is approved only for ulcerative colitis and is not approved at all for rheumatoid arthritis or psoriatic arthritis. (1) (5)

Why does the US label list no contraindications while the UK label lists several?

This is a real, verified difference between the current labels reviewed. The current US FDA label explicitly states 'Contraindications: None.' The UK SmPC, by contrast, lists active tuberculosis or serious infection, severe hepatic impairment, and pregnancy/lactation as absolute contraindications. Always follow the product information and prescriber guidance specific to your own country. (1) (2)

Am I at higher risk if I am 65 or older, or if I smoke?

Yes, based on real, specific regulatory findings. In the EU, regulators (via the EMA's Pharmacovigilance Risk Assessment Committee) recommended that tofacitinib be used in patients 65 and older, current or past smokers, or those with other cardiovascular or malignancy risk factors only if no suitable treatment alternative is available. Discuss your individual risk factors with your prescriber. (3)

What is the mechanism of action of tofacitinib (as citrate)?

Tofacitinib is an oral small-molecule inhibitor of Janus kinases (JAK), predominantly JAK1 and JAK3, with functional selectivity over JAK2. Inhibition of JAK1 and JAK3 by tofacitinib attenuates signalling by multiple cytokines involved in the inflammatory and immune response, including interleukins and interferons. (1) (2)

What is the generic name of Xeljanz (Xeljanz XR)?

The generic name is tofacitinib (as citrate). (1) (2)

What class of drug is tofacitinib (as citrate)?

Xeljanz (Xeljanz XR) is classed as: Janus kinase (JAK) inhibitor. (1) (2)

References

  1. XELJANZ (tofacitinib) tablets, oral solution / XELJANZ XR (tofacitinib) extended-release tablets -- full prescribing information, revised 3/2026, boxed warning updated 10/2025U.S. Food and Drug Administration / DailyMed (NIH), full prescribing information, Pfizer Inc. · United States · accessed 2026-07-31 · source 1
  2. XELJANZ 5 mg film-coated tablets -- Summary of Product Characteristics (SmPC), last updated 16 Mar 2026electronic medicines compendium (emc), United Kingdom -- Pfizer Ltd · United Kingdom · accessed 2026-07-31 · source 2
  3. Xeljanz (tofacitinib): increased risk of major adverse cardiovascular events and malignancies with use of tofacitinib relative to TNF-alpha inhibitors -- Direct Healthcare Professional Communication (DHPC)European Medicines Agency (EMA), Direct Healthcare Professional Communication / PRAC recommendation · European Union · accessed 2026-07-31 · source 3
  4. XELJANZ/XELJANZ XR (tofacitinib citrate) -- Product MonographHealth Canada / Pfizer Canada Inc., Product Monograph · Canada · accessed 2026-07-31 · source 4
  5. XELJANZ XR tofacitinib (as citrate) 11 mg extended-release tablet -- ARTG entries 381790/381810; XELJANZ oral solution -- ARTG 386772; TGA safety alert on tofacitinibTherapeutic Goods Administration (TGA), Australia · Australia · accessed 2026-07-31 · source 5
  6. Tofacitinib Devatis 5 mg Film Coated Tablets -- New Zealand Data SheetMedsafe (New Zealand regulator) -- official New Zealand Data Sheet (generic: Tofacitinib Devatis) · New Zealand · accessed 2026-07-31 · source 6

Brand names by country

Single-ingredient tofacitinib (as citrate) names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.

Priority countries

United States

  • XELJANZ11 mg, 10 mg, 22 mg, 5 mg, 1 mg/mL · pfizer laboratories div pfizer inc

United Kingdom

  • XELJANZ (2)current licensed product · 5 mg, 10 mg film-coated tablet, 1 mg/mL oral solution · Pfizer Ltd
  • XELJANZ (2)current licensed product · 11 mg prolonged-release tablet · Pfizer Ltd

Canada

  • XELJANZ

Australia

  • XELJANZ XR (5)current register product · 11 mg extended-release tablet · Pfizer Australia Pty Ltd
  • XELJANZ (5)current register product · 1 mg/mL oral solution · Pfizer Australia Pty Ltd

New Zealand

  • Tofacitinib Devatis (6)current registered product · 5 mg film-coated tablet · See current Medsafe data sheet
View brands in additional countries.

European Union

Xeljanz (centrally monitored, subject to a formal EU pharmacovigilance restriction) (3)

This page provides general reference information about Xeljanz (tofacitinib) and is not a substitute for advice from the prescriber managing your treatment. All dosing and treatment decisions should be made with your prescriber, especially given the real market-specific differences in dosing limitations and contraindications described above.

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