Tofacitinib Citrate (Xeljanz®)

Pill Bottle with Pills

Tofacitinib (Xeljanz®) is an oral, small molecule drug used to treat adults with moderately to severely active rheumatoid arthritis (RA) in which methotrexate did not work well. 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.

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 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. 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 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 Doctor

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 doctor. Notify your doctor if you become pregnant or are planning pregnancy, or if you are breastfeeding. Be sure to talk with your doctor 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. These include the shingles vaccine, the nasal spray flu vaccine, and others such as the measles, mumps, rubella, and yellow fever vaccines.

Updated July 2017 by Paul Sufka, MD 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.

© 2017 American College of Rheumatology