Tofacitinib Citrate (Xeljanz)


Tofacitinib Citrate (Xeljanz) is an oral drug used to treat adults with moderate to severe active rheumatoid arthritis (RA), active psoriatic arthritis, ankylosing spondylitis, moderate to severe ulcerative colitis, and children ages 2 and older with active polyarticular juvenile idiopathic arthritis. It works by blocking enzymes 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 and tumor necrosis factor inhibitors.

How To Take It

Tofacitinib is a pill that is taken either as 5 mg twice a day (Xeljanz) or as 11 mg once per day (Xeljanz XR). 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 for 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 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. 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. Tell your doctor if you become pregnant or are planning pregnancy, or if you are breastfeeding. 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 receiving any vaccines or undergoing any surgeries while taking this medication. Avoid live vaccines like the nasal spray flu vaccine, and others such as the measles, mumps, rubella, and yellow fever vaccines.

Updated February 2024 by Karmela Kim Chan, MD, 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.

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