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Xeljanz (tofacitinib)

Xeljanz (tofacitinib) is a prescription medicine recommended for adults with moderately to severely active ulcerative colitis (UC). It is the only FDA approved oral medication for the treatment of adults with this condition. Manufactured by Pfizer, it came to market in 2012 and was approved for UC in June 2018. It is sold in the United States under the brand name Xeljanz.

How does tofacitinib work?

Tofacitinib works as a Janus kinase (JAK) inhibitor. JAKs are enzymes, proteins, found in many cells in the body including stem cells, bones, and joints.1,2,3,4 They regulate the signals that help to activate the body’s immune response system. Tofacitinib inhibits JAK-1 and JAK-3, which helps block receptors that otherwise, can trigger inflammation. 1,2,3

By repressing JAKs, inhibiting the activation T and B cells, the inflammatory process that can cause arthritis and UC can be slowed or stopped. Left uncontrolled, the inflammation can bring about the symptoms of ulcerative colitis. By blocking proteins that trigger this inflammation, tofacitinib can benefit some people with moderate-to-severe ulcerative colitis by:

  • Reducing the symptoms of UC in as little as two weeks
  • Helping to improve the appearance of the intestinal lining
  • Providing sustained steroid-free remission

Tofacitinib comes in 3 forms: 5 mg and 10 mg tablets and 11 mg XR (extended release) tablets. Tablets should be swallowed whole and intact, they should not be crushed, split, or chewed1,2. For people with ulcerative colitis, it is taken orally two times a day with or without food. The initial dose is 10 mg twice daily for at least 8 weeks. A doctor will then adjust the dosage as needed to 5 mg or 10 mg twice daily to the lowest effective dose. A recommendation may be made to discontinue tofacitinib if no therapeutic effect has been achieved after 16 weeks. For people with severe kidney or liver impairment, the recommended dosage is half the standard dosage. People with ulcerative colitis should not take the XR formulation. 1,2

Who can take tofacitinib?

Tofacitinib is approved in the United States for treating adults with moderate to severely active UC. It can also be prescribed for people who have rheumatoid arthritis and psoriatic arthritis. It is not known if this medication is safe and effective in children or in people with Hepatitis B or C. 1,2,3

Before prescribing tofacitinib, healthcare providers need to know about any medicines or supplements that the patient is taking. Women who are pregnant, planning to become pregnant, or breastfeeding should also inform their healthcare providers. Your doctor should test you for tuberculosis (TB) before starting and while undergoing treatment with tofacitinib.

People taking tofacitinib may be at a higher risk of developing shingles (herpes zoster). If the higher dose (10 mg twice daily) is prescribed there is an increased risk of serious infections and shingles.1,2

People who are taking tofacitinib should not receive any kind of live vaccines during treatment but can receive non-live vaccines. It is a good idea to make sure all vaccinations are up to date before initiating treatment.

Because of some side effects linked to tofacitinib, healthcare providers need to know if the patient currently has any type of infection, tends to get infections often, or has recurring infections. They also need to know if the patient has, or has ever had: 1,2,3

  • Tuberculosis, or has been near someone with TB
  • Diabetes
  • HIV or other Immune system problems
  • Hepatitis B or C or other liver problems
  • Cancer
  • Chronic lung disease
  • Diverticulitis or stomach ulcers
  • Live in or travel to areas where there is an increased risk of fungal infections

What side effects are linked to tofacitinib?

The most common side effects experienced by people who take tofacitinib are:1,2,3

  • Nasal congestion, sore throat, and runny nose
  • Upper respiratory or sinus infections
  • Headache
  • Increased cholesterol levels
  • Increased muscle enzyme levels
  • Rash
  • Diarrhea
  • Shingles (herpes zoster)

Tofacitinib changes the way the body’s immune system works. Risks for developing lymphoma and other cancers can increase when taking tofacitinib, including skin cancers. People may also be more likely to develop infections and have more difficulty fighting them off. These can include serious viral, bacterial, or fungal infections, including tuberculosis.1,2,3

Healthcare providers will carefully monitor patients taking tofacitinib for any serious side effects including:

  • Stomach perforations (ulcers) Heart failure
  • Serious Infections
  • Changes in certain lab test results including blood cell counts and liver enzymes
  • Lymphoma
  • Skin cancer

This is not a complete list of side effects. Patients should let their healthcare providers know right away if they have any new symptoms, symptoms that are unusually severe, or symptoms that persist.1,2,3,4

New warnings

At the end of July 2019, the FDA approved new warnings about the increased risk of blood clots and added a Boxed Warning for the medication. The approved use of tofacitinib for ulcerative colitis will also be limited to certain patients who are not treated effectively or who experience severe side effects with certain other medicines.5

Written by: Linda Saxl Minton | Last Reviewed: May 2019.
  1. Prescribing Information. Available at: http://labeling.pfizer.com/ShowLabeling.aspx?id=959. Accessed 3.10.19
  2. Prescribing Information. Available at: http://labeling.pfizer.com/ShowLabeling.aspx?id=959§ion=MedGuide. Accessed 3.10.19
  3. What is Xeljanz. Available at: https://uc.xeljanz.com/. Accessed 3.10.19 https://uc.xeljanz.com/important-safety-information. Accessed 3.10.19
  4. What You Need to Know About Xeljanz. Available at: https://www.verywellhealth.com/what-you-need-to-know-about-xeljanz-tofacitinib-4171527. Accessed 3.10.19
  5. U.S. Food & Drug Administration, MedWatch: The FDA Safety Information and Adverse Event Reporting Program. (2019, July 26). Xeljanz, Xeljanz XR (tofacitinib): Drug Safety Communication - Due to an Increased Risk of Blood Clots and Death with Higher Dose [Press release]. Retrieved July 29, 2019, from https://www.fda.gov/safety/medwatch-safety-alerts-human-medical-products/xeljanz-xeljanz-xr-tofacitinib-drug-safety-communication-due-increased-risk-blood-clots-and-death?utm_campaign=FDA Medatch Xeljanz, Xeljanz XR (tofacitinib): Drug Safety Communication&utm_medium=email&utm_source=Eloqua