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Tofacitinib Citrate (Xeljanz)


Tofacitinib Citrate (Xeljanz) is an oral, small molecule drug used to treat adults with moderate to severe active rheumatoid arthritis (RA), active psoriatic arthritis, moderate to severe ulcerative colitis, ankylosing spondylitis, and children ages 2 an older with active polyarticular juvenile idiopathic arthritis. Tofacitinib works by blocking the body’s production of enzymes called Janus kinases (JAKs). JAKs play a role in joint inflammation in RA, which can cause pain, swelling, and stiffness. This medication is most commonly used after methotrexate and tumor necrosis factor (TNF) inhibitors.

How to Take It

Tofacitinib is a pill that is taken either as 5 mg twice per day (Xeljanz) or as 11 mg once per day (Xeljanz XR). You may take tofacitinib tablets with or without food. People with moderate to severe renal impairment or moderate hepatic impairment should take only one 5 mg tablet per day. 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

Tofacitinib can lower the ability of your immune system to fight infections. If you develop symptoms of an infection while using this medication, you should stop it and contact your doctor. On September 1, the FDA placed a boxed warning on tofacitinib, baricitinib, and upadacitinib due to data demonstrating increased risk of MACE (major adverse cardiac event), malignancy, thrombotic events, and mortality when tofacitinib was compared to TNFi in long-term surveillance data. In addition, the FDA adjusted the indications for the use of these JAK inhibitors, making them approved for TNF inhibitor inadequate response or intolerance. On January 27, 2022, the ORAL surveillance study was published and the data behind the changes were released.

Read the ACR Statement on JAK Inhibitor Boxed Warning

The most common side effects of tofacitinib are upper respiratory tract infections, headache, diarrhea, and nasopharyngitis. The most common side effects of tofacitinib are upper respiratory tract infections, headache, diarrhea, and nasopharyngitis. Other serious side effects include herpes zoster and blood clots. 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 risk of reactivation of these infections. Tofacitinib has been associated with increased cholesterol levels in some patients and should be periodically monitored. If your cholesterol level becomes too high, it is possible you may need to start taking a medication to lower it. A rare complication seen with tofacitinib use in clinical trials was bowel perforation, or a hole in the bowel wall. If you have a history or diverticulitis or develop abdominal pain or bloody bowel movements while taking tofacitinib, you should notify your doctor immediately. Lymphoma and other malignancies have been observed in patients treated with tofacitinib. Epstein Barr Virus-associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with tofacitinib and concomitant immunosuppressive medications.

Tell Your Rheumatology Provider

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 rheumatology provider. Notify your doctor if you become pregnant or are planning pregnancy, or if you are breastfeeding. Be sure to talk with your rheumatology provider before receiving any vaccines or undergoing any surgeries while taking this medication. Live vaccines should be avoided while on this medication and you should discuss updating your vaccinations prior to starting this medication. Live vaccines contain a milder form of the virus or bacteria to help your body develop an immune response without you developing symptoms of the disease it is intended to prevent. These vaccines always carry a small chance a person could get the infection from the vaccine. Live vaccines include the nasal spray flu vaccine, and others such as the measles, mumps, rubella, and yellow fever vaccines.

Updated February 2022 by Senada Arabelovic, DO, and reviewed by the American College of Rheumatology Committee on Communications and Marketing.

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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