Tofacitinib

Drug Name
Tofacitinib

Brand Name(s)
Xeljanz®

Drug Class
Janus Kinase (JAK) Inhibitor

Tofacitinib is a DMARD used to treat inflammatory types of arthritis, such as rheumatoid arthritis (RA).

  • What types of arthritis is tofacitinib used for?

    Tofacitinib is a DMARD used to treat inflammatory types of arthritis, such as rheumatoid arthritis (RA).

    Tofacitinib is recommended for use in combination with methotrexate (MTX) in adult patients with moderate to severely active RA who have had an inadequate response to MTX. For patients who cannot tolerate MTX, tofacitinib may be given as monotherapy.

    Tofacitinib is never used in combination with biologic medications. Combining tofacitinib with biologic therapy is not recommended because of the increased risk for infection.

  • How is tofacitinib administered?

    Tofacitinib is taken orally in pill form.

  • What is the typical dose and when do I take it?

    Tofacitinib is available in 5 mg tablets. The usual dose is one tablet twice daily. Your prescriber may reduce the dose if you have liver or kidney problems.

  • How long will it take to work?

    Like many of the DMARDs, you will not feel the effects of tofacitinib right away. Most people may start noticing the effects about two to eight weeks after they start taking the medication, but full benefits may not occur for three to six months. It is important to be patient and keep taking your medication.

  • When should I not take tofacitinib and call my doctor?

    Tofacitinib can make it harder for your body to fight infections. Therefore, if you have a fever or think you may have an infection, contact your health-care provider immediately. Also contact your prescriber if you are having surgery as you may need to stop tofacitinib until you are healed and there is no sign of infection.

    Before taking tofacitinib, tell your health-care provider if you are pregnant or planning to become pregnant or are breastfeeding or planning to breastfeed. Women should not breastfeed while being treated with tofacitinib.

    Ideally your vaccinations should be up to date prior to starting tofacitinib. If you have already started therapy with tofacitinib, most inactive vaccines are recommended, if indicated (e.g., influenza, pneumococcal). Live vaccines are not recommended due to risk of causing infection. Please speak with your health-care providers about vaccinations before starting tofacitinib.

    Anyone who has had a previous allergic reaction to tofacitinib should avoid the medication.

    Tofacitinib interacts with a number of other medications. Please speak with your health-care provider about whether any of the other medications you currently take interact with tofacitinib. It is also recommended that you avoid grapefruit juice and St. John’s wort while taking tofacitinib.

    Your body may harbour the bacteria that can cause tuberculosis (TB) if you have been exposed to TB in the past. You may not know you are carrying TB as the bacteria remain in an inactive state and cause no symptoms. This is known as latent TB infection (LTBI). People with LTBI are not infectious and cannot spread TB to others. Tofacitinib can increase the risk of reactivation of LTBI. Prior to starting tofacitinib therapy, your prescriber will screen for LTBI. If you test positive you will be required to take an anti-TB medication prior to starting tofacitinib. Please speak with your health-care provider about LTBI screening before starting a tofacitinib.

    Tofacitinib has been rarely associated with a small increased risk of developing certain types of cancer. Proof of a link between tofacitinib and the development of cancer is difficult as people with inflammatory arthritis are generally at a higher risk of developing certain cancers, as compared to the general population. The role of tofacitinib in the development of cancer is currently unknown. Please speak with your health-care provider if you have any questions.

  • What are the side effects of tofacitinib?

    Like all medications, taking tofacitinib carries some risk of side effects, which must be balanced with the potential benefits. In general, the risk of joint damage and permanent disability (resulting from arthritis) is much greater than the risks of side effects from tofacitinib. When monitored properly the vast majority of side effects are rare, most improve over time and are reversible.

    The most common side effects of tofacitinib are nausea, indigestion and diarrhea. Some people also experience headaches, high blood pressure, urinary tract infections and upper respiratory tract infections.

    Tofacitinib may affect your blood counts, liver or kidney function and cholesterol levels. Your health-care provider will use blood tests to monitor for these changes.

    In rare cases, tofacitinib has been associated with stomach perforations (holes in the lining of the stomach). All patients who developed stomach perforations were also taking NSAIDs and/or corticosteroids. However, the contribution of these medications to the development of stomach perforations is not known. Tofacitinib should be used with caution in patients who may be at increased risk for stomach perforation (e.g., using NSAIDs and/or corticosteroids, people with a history of diverticulitis). Stomach perforations require immediate medical attention. If you develop fever and severe stomach pain that does not go away, seek medical attention.

  • What helps to reduce side effects?

    Take tofacitinib as prescribed and contact your health-care provider if you have any concerns while taking the medication.

    Taking tofacitinib with food may help reduce nausea and stomach upset.

  • Do I need any monitoring while taking tofacitinib?

    You will need blood tests every one to three months. This is important to ensure the tofacitinib is having no harmful effects on your blood counts, liver, kidneys or cholesterol levels.


This information was last updated November 2017, with expert advice from:

Jason Kielly, B.Sc. (pharm.), Pharm.D.
Assistant Professor, School of Pharmacy, Memorial University of Newfoundland
Clinical Pharmacist, Rheumatic Health Program, Eastern Health

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