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Xeljanz XR Side Effects

Generic name: tofacitinib

Medically reviewed by Philip Thornton, DipPharm. Last updated on Apr 27, 2022.

Note: This document contains side effect information about tofacitinib. Some dosage forms listed on this page may not apply to the brand name Xeljanz XR.

Summary

Common side effects of Xeljanz XR include: infection. Other side effects include: diarrhea and headache. Continue reading for a comprehensive list of adverse effects.

Applies to tofacitinib: oral solution, oral tablets.

Warning

    Serious Infections
  • Serious, sometimes fatal infections including tuberculosis (pulmonary or extrapulmonary disease), bacterial and viral infections, invasive fungal infections (may be disseminated), and other opportunistic infections reported.1 3 4 5

  • Carefully consider risks and benefits prior to initiating tofacitinib therapy in patients with chronic or recurring infections.1

  • Evaluate patients for latent tuberculosis infection prior to and periodically during tofacitinib therapy; if indicated, initiate appropriate antimycobacterial regimen prior to initiating tofacitinib therapy.1

  • Closely monitor patients for infection, including active tuberculosis in those with a negative test for latent tuberculosis, during and after treatment.1 If serious infection develops, interrupt tofacitinib until infection is controlled.1

    Mortality
  • Higher overall mortality rate, including sudden cardiovascular death, reported with tofacitinib 5 or 10 mg twice daily compared with a TNF blocking agent in a postmarketing safety study in rheumatoid arthritis patients ≥50 years of age with ≥1 cardiovascular risk factor.1 27 Tofacitinib dosage of 10 mg twice daily (as conventional tablets or oral solution) or 22 mg once daily (as extended-release tablets) is not recommended for the treatment of rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis.1

    Malignancies
  • Lymphoma and other malignancies (excluding nonmelanoma skin cancer) reported at a higher rate with tofacitinib 5 or 10 mg twice daily compared with TNF blocking agents in patients with rheumatoid arthritis.1 Risk of lymphomas and lung cancers were also increased with tofacitinib 5 or 10 mg twice daily compared with TNF blocking agents; patients who are current or past smokers are at additional risk.1

  • Increased incidence of Epstein Barr virus-associated lymphoproliferative disorder observed in renal allograft recipients receiving tofacitinib and concomitant immunosuppressive agents.1

    Major Adverse Cardiovascular Events
  • Higher rate of major adverse cardiovascular events reported with tofacitinib 5 or 10 mg twice daily compared with TNF blocking agents in a postmarketing safety study in patients with rheumatoid arthritis ≥50 years of age with ≥1 cardiovascular risk factor.1 Patients who are current or past smokers are at additional risk.1

  • Discontinue tofacitinib in patients who experience MI or stroke.1

    Thrombosis
  • Thromboembolic events, (i.e., PE, DVT, arterial thrombosis), sometimes serious or fatal, reported in patients receiving tofacitinib or other Janus kinase inhibitors for inflammatory conditions.1

  • Higher incidence of thromboembolic events reported with tofacitinib 10 mg twice daily compared with either tofacitinib 5 mg twice daily or a TNF blocking agent in a postmarketing safety study in rheumatoid arthritis patients ≥50 years of age with ≥1 cardiovascular risk factor.1 27

  • Discontinue tofacitinib and promptly evaluate patient if symptoms of thrombosis occur.1 27

  • In patients with ulcerative colitis, use tofacitinib at lowest effective dosage and for shortest duration needed to achieve and maintain response.1 27

Side effects include:

Rheumatoid arthritis patients receiving tofacitinib (the active ingredient contained in Xeljanz XR) 5 or 10 mg twice daily monotherapy or in combination with DMARDs (≥2%): Diarrhea, headache, nasopharyngitis, upper respiratory tract infection.

Psoriatic arthritis and ankylosing spondylitis: Adverse effects similar to those observed in patients with rheumatoid arthritis.

Ulcerative colitis (≥5%): Nasopharyngitis, elevated cholesterol concentrations, headache, upper respiratory tract infection, increased blood creatine kinase (CK, creatine phosphokinase, CPK) concentrations, rash, diarrhea, herpes zoster.

Polyarticular-course JIA: Adverse effects generally consistent with those reported in adults with rheumatoid arthritis.

For Healthcare Professionals

Applies to tofacitinib: oral solution, oral tablet, oral tablet extended release.

General

In rheumatoid arthritis clinical trials, the most common serious adverse reactions were serious infections; the most common serious infections included pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis. In ulcerative colitis induction and maintenance trials, the most common serious adverse reaction was worsening of ulcerative colitis.[Ref]

Cardiovascular

Common (1% to 10%): Hypertension

Uncommon (0.1% to 1%): Venous thromboembolism (includes pulmonary embolism, deep vein thrombosis), myocardial infarction

Frequency not reported: Deep vein thrombosis, nonfatal myocardial infarction, fatal myocardial infarction, arterial thromboembolism, major adverse cardiovascular events (includes nonfatal myocardial infarction, nonfatal stroke, cardiovascular death [excluding fatal pulmonary embolism]), thrombosis (including pulmonary embolism, deep venous thrombosis, arterial thrombosis), decreased heart rate, prolonged PR interval

Dermatologic

Common (1% to 10%): Rash, acne

Uncommon (0.1% to 1%): Erythema, pruritus, cellulitis, herpes simplex

Frequency not reported: Multidermatomal herpes zoster, pilonidal cyst

Postmarketing reports: Angioedema, urticaria

Gastrointestinal

Common (1% to 10%): Diarrhea, abdominal pain, dyspepsia, vomiting, gastritis, nausea, constipation, gastroenteritis, upper abdominal pain, ulcerative colitis

Uncommon (0.1% to 1%): Diverticulitis, viral gastroenteritis, appendicitis

Frequency not reported: Esophageal candidiasis, worsening of ulcerative colitis, gastrointestinal perforation, gastrointestinal obstruction

Genitourinary

Common (1% to 10%): Urinary tract infection

Uncommon (0.1% to 1%): Pyelonephritis

Rare (0.01% to 0.1%): Urosepsis

Hematologic

Common (1% to 10%): Anemia, decreased absolute lymphocyte count

Uncommon (0.1% to 1%): Leukopenia, neutropenia, lymphopenia

Rare (0.01% to 0.1%): Decreased absolute neutrophil count

Frequency not reported: Lymphocytosis

Hepatic

Common (1% to 10%): Increased AST, increased ALT, increased GGT

Uncommon (0.1% to 1%): Hepatic steatosis, increased hepatic enzymes, increased transaminases, abnormal liver function test

Frequency not reported: Drug-induced liver injury, increased bilirubin

Postmarketing reports: Hepatitis B reactivation

Hypersensitivity

Postmarketing reports: Hypersensitivity/allergic reactions, drug hypersensitivity (e.g., angioedema, urticaria)

Metabolic

Common (1% to 10%): Hypercholesterolemia

Uncommon (0.1% to 1%): Dehydration, dyslipidemia, hyperlipidemia

Musculoskeletal

Common (1% to 10%): Rheumatoid arthritis, back pain, arthralgia, increased blood creatine phosphokinase

Uncommon (0.1% to 1%): Musculoskeletal pain, tendonitis, joint swelling, ligament sprain, muscle strain

Rare (0.01% to 0.1%): Necrotizing fasciitis, bacterial arthritis

Frequency not reported: Limb abscess, fractures

Nervous system

Common (1% to 10%): Headache, dizziness

Uncommon (0.1% to 1%): Paresthesia

Rare (0.01% to 0.1%): Tuberculosis of central nervous system, encephalitis, cryptococcal meningitis

Frequency not reported: Aseptic meningitis, epidural empyema (with sinusitis and subperiosteal abscess)

Oncologic

Common (1% to 10%): Epstein Barr Virus-associated posttransplant lymphoproliferative disorder

Uncommon (0.1% to 1%): Lung cancer, nonmelanoma skin cancer (includes basal cell carcinoma, squamous cell carcinoma)

Rare (0.01% to 0.1%): Lymphoma

Frequency not reported: Solid cancers, malignancies (including solid cancers, lymphomas, nonmelanoma skin cancer, lung cancer, breast cancer, gastric cancer, colorectal cancer, renal cell cancer, prostate cancer, malignant melanoma), basal cell carcinoma, cutaneous squamous cell carcinoma, breast cancer, melanoma, prostate cancer, pancreatic cancer

Other

Very common (10% or more): Infections (up to 49.4%)

Common (1% to 10%): Pyrexia, fatigue, peripheral edema, herpes zoster, increased weight, fall, increased cholesterol levels (includes hypercholesterolemia, hyperlipidemia, increased blood cholesterol, dyslipidemia, increased blood triglycerides, increased low-density lipoprotein [LDL], abnormal LDL, increased lipids), increased blood cholesterol, serious infections

Uncommon (0.1% to 1%): Tuberculosis, viral infection, increased LDL

Rare (0.01% to 0.1%): Sepsis, disseminated tuberculosis, bacteremia, staphylococcal bacteremia, atypical mycobacterial infection, CMV infection, Mycobacterium avium complex infection

Frequency not reported: Opportunistic infections, other mycobacterial infections, cryptococcus, histoplasmosis, BK virus infection, listeriosis, increased lipid parameters (total cholesterol, LDL cholesterol, high-density lipoprotein [HDL] cholesterol, triglycerides), increased LDL cholesterol, increased HDL cholesterol, septic shock, opportunistic herpes zoster infections (including meningoencephalitis, ophthalmologic, disseminated cutaneous), viral reactivation (including herpes virus reactivation [e.g., herpes zoster]), all-cause mortality (including sudden cardiovascular death), deaths associated with infection, deaths associated with cardiovascular events, deaths associated with malignancies, deaths associated with other causes (excluding infections, cardiovascular events, malignancies), dissemination of the vaccine strain of varicella zoster virus

A patient had dissemination of the vaccine strain of varicella zoster virus, 16 days after vaccination with live attenuated virus vaccine and 2 days after starting therapy with 5 mg twice a day; the patient was varicella virus naive, as shown by no history of varicella infection and no anti-varicella antibodies at baseline. This drug was discontinued and the patient recovered after treatment with standard doses of antiviral therapy.

Psychiatric

Uncommon (0.1% to 1%): Insomnia

Renal

Uncommon (0.1% to 1%): Increased blood creatinine

Frequency not reported: Escherichia pyelonephritis

Respiratory

Very common (10% or more): Nasopharyngitis (up to 18.2%)

Common (1% to 10%): Pneumonia, influenza, sinusitis, pharyngitis, upper respiratory tract infections, bronchitis, cough, viral upper respiratory tract infection

Uncommon (0.1% to 1%): Dyspnea, sinus congestion

Rare (0.01% to 0.1%): Pneumocystis jirovecii pneumonia, pneumococcal pneumonia, bacterial pneumonia

Frequency not reported: Pulmonary embolism, interstitial lung disease

Frequently asked questions

References

1. "Product Information. Xeljanz (tofacitinib)." Pfizer U.S. Pharmaceuticals Group (2021):

2. "Product Information. Xeljanz XR (tofacitinib)." Pfizer U.S. Pharmaceuticals Group (2021):

3. "Product Information. Xeljanz (tOFACitinib)." Pfizer Australia Pty Ltd (2021):

4. "Product Information. Xeljanz (tofacitinib)." Pfizer Ltd (2022):

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Some side effects may not be reported. You may report them to the FDA.