Tofacitinib Citrate (Xeljanz)
Tofacitinib Citrate (Xeljanz) is an oral drug used to treat adults with moderately-severely active rheumatoid arthritis, active psoriatic arthritis, ankylosing spondylitis, moderate to severe ulcerative colitis, and polyarticular juvenile idiopathic arthritis among other diseases. It works by blocking proteins called Janus kinases (JAKs). JAKs play a role in joint inflammation, which can cause pain, swelling, and stiffness. This medication is often used if a patient has not had a good response to other medications such as methotrexate or tumor necrosis factor inhibitors.
How To Take It
Tofacitinib is a pill that is most often prescribed to take as 5 mg pill twice a day (Xeljanz) or as 11 mg pill once per day (Xeljanz XR). Sometimes, there is a higher dose prescribed at the start of therapy (induction dose). You may take tofacitinib with or without food. People with moderate to severe kidney or liver problems should take a lower dose. Tofacitinib may be used alone or in combination with methotrexate or other disease modifying antirheumatic drugs (DMARDs). Tofacitinib should not be given in combination with another biologic drug or other potent immunosuppressants such as azathioprine or mycophenolate. Some patients will start to see improvement within a few weeks, but it may take several months to take full effect. Blood tests will be used to monitor increases in cholesterol or liver enzymes and for reductions in blood cell counts while taking tofacitinib.
Side Effects
The most common side effects of tofacitinib are upper respiratory tract infections, headache, diarrhea, and nasopharyngitis. All patients should be tested for tuberculosis before starting on tofacitinib. Patients should also be screened for hepatitis B and C prior to starting tofacitinib, since this medication may increase the risk of reactivation of these infections. Tofacitinib increases your chance of getting viral infections such as shingles. In patients over 65 years of age, tofacitinib has been linked to heart attacks, strokes, and blood clots. It can raise your cholesterol levels. Rarely, it may cause colon perforation (rupture of your gut). Lymphoma and other malignancies have been observed in patients treated with tofacitinib.
Tell Your Rheumatology Provider
Let your doctor know if you have a history of diverticulitis and other serious infections. Ask your doctor about getting appropriate vaccines before starting the drug, including the shingles vaccine and avoid live vaccines like the nasal spray flu vaccine, and others such as the measles, mumps, rubella, and yellow fever vaccines while being on tofacitinib. If you develop symptoms of an infection such as a fever or cough or think you are having any side effects (especially abdominal pain, bloody bowel movements, or allergic reactions), contact your rheumatologist. Be sure to talk with your doctor before undergoing any surgeries while taking this medication. Tell your doctor if you become pregnant or are planning for a pregnancy, or if you are breastfeeding.
Updated April 2025 by Pankti Reid, MD, MPH, and reviewed by the American College of Rheumatology Communications and Marketing Committee.
This information is provided for general education only. Individuals should consult a qualified health care provider for professional medical advice, diagnosis and treatment of a medical or health condition.