Xeljanz (Tofacitinib) – Oral

Warning:

The Food and Drug Administration (FDA) issued a few warning statements for Xeljanz (tofacitinib).

Xeljanz use can increase the risk of serious infections, including tuberculosis (TB), leading to hospitalization or death. You may be tested for TB before and during therapy. If you have TB, it must be treated before you start taking Xeljanz.

Xeljanz, which is a Janus kinase (JAK) inhibitor, also has a higher rate of all-cause mortality, including sudden cardiovascular death, than tumor necrosis factor (TNF) inhibitors in people with rheumatoid arthritis (RA), with at least one heart risk factor.

In clinical studies, people taking Xeljanz have developed malignancies, including lymphomas and solid cancers. A higher rate of lymphomas and lung cancers occurs with Xeljanz use vs. TNF inhibitor use in people with RA.

Lastly, Xeljanz and other JAK inhibitors have been associated with thrombosis (blood clots) in some people.

What Is Xeljanz?

Xeljanz (tofacitinib) is an oral Janus kinase (JAK) inhibitor used to treat certain types of arthritis and other inflammatory conditions.

JAK inhibitors are a group of medications that interfere with the activity of enzymes called Janus kinases, which send signals to cells in the immune system. These enzymes play an important role in different inflammatory and autoimmune diseases. Drugs like Xeljanz can treat diseases in which an overactive immune system attacks the body’s tissues by inhibiting the activity of JAK molecules.

Xeljanz is available in tablet, extended-release tablet (Xeljanz XR), and liquid (solution) form.

Drug Facts

Generic Name: Tofacitinib

Brand Name(s): Xeljanz, Xeljanz XR

Drug Availability: Prescription

Administration Route: Oral

Therapeutic Classification: Antirheumatic

Available Generically: No

Controlled Substance: N/A

Active Ingredient: Tofacitinib citrate

Dosage Form(s): Tablet, liquid

What Is Xeljanz Used For?

Xeljanz helps treat certain types of arthritis and inflammatory conditions in people who have already tried treatment with tumor necrosis factor (TNF) inhibitors.

The Food and Drug Administration (FDA) approved Xeljanz to treat adults with:

  • Moderate to severe rheumatoid arthritis (RA)
  • Active psoriatic arthritis (PsA)
  • Ankylosing spondylitis
  • Ulcerative colitis (UC)

The liquid formulation is also approved for people 2 years and older with active polyarticular (i.e., affecting multiple joints) juvenile idiopathic arthritis.

Xeljanz (Tofacitinib) Drug Information - Image of a man and part of his immune system

Verywell / Zoe Hansen

How to Take Xeljanz

Use Xeljanz exactly as prescribed by your healthcare provider. They will instruct you on when and how to take this medication. The formulation and dose may be individualized based on the condition you are being treated for and other factors.

However, there are a few general tips to follow:

  • You can take Xeljanz tablets or the oral solution with or without food.
  • If taking the extended-release formulation, don’t crush, split, or chew the tablets.
  • Take the oral solution using the press-in bottle adapter and oral dosing syringe included with the medication.
  • Xeljanz oral solution and Xeljanz XR (extended-release formulation) are not interchangeable.

For UC specifically, treatment with Xeljanz is often divided into two types of therapy:

  • Induction therapy, which refers to the first stage of therapy
  • Maintenance therapy, which describes therapy intended to sustain a treatment response

This can be highly individualized, depending on how you respond to treatment. A typical induction schedule would be Xeljanz 10 milligrams (mg) twice daily (or Xeljanz XR 22 milligrams once daily) for eight to 16 weeks. This is followed by maintenance treatment with Xeljanz 5 milligrams, twice daily, or Xeljanz XR 11 milligrams, once daily. If your ulcerative colitis symptoms flare up during treatment, your healthcare provider may consider a short burst with an increased dose to bring you back to your baseline.

If you are taking Xeljanz XR, you may see a portion of the tablet in your stool. This is normal and doesn’t mean that the drug will not be effective.

Storage

Store Xeljanz tablets and oral solution at room temperature (68 to 77 degrees Fahrenheit). The oral solution is dispensed in bottles, and the package includes a medication syringe and a bottle adapter to draw up the liquid. Keep the solution in its original bottle and carton away from light, as exposure may affect the medication. Throw away any unused solution after 60 days.

Off-Label Uses

Healthcare providers can prescribe drugs “off-label” for conditions not specifically mentioned in the product label. Several off-label uses for Xeljanz are being studied.

The JAK molecules targeted by Xeljanz may have a role in multiple inflammatory and autoimmune diseases. Researchers have looked at whether Xeljanz can be effective in treating various rheumatic conditions (e.g., dermatomyositis, polymyositis, or lupus) and autoimmune skin diseases (e.g., atopic dermatitis, alopecia areata, and plaque psoriasis).

Early data suggest that Xeljanz may benefit people with these conditions, especially if they have not responded to other therapies. However, more study is needed before Xeljanz is widely used for these conditions.

Xeljanz is also being studied for use in hospitalized people with COVID-19. The National Institutes of Health recommends using tofacitinib in certain individuals who require supplemental oxygen if Olumiant (baricitinib), another JAK inhibitor, is unavailable. Dosing is recommended as 10 milligrams twice daily for up to 14 days or until hospital discharge. However, it must be given in combination with dexamethasone with or without remdesivir.

How Long Does Xeljanz Take to Work?

In clinical trials, people who responded to Xeljanz noted an improvement in their rheumatoid arthritis symptoms within the first 12 weeks (three months) of starting treatment.

What Are the Side Effects of Xeljanz?

This is not a complete list of side effects and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your healthcare provider. You may report side effects to the FDA at fda.gov/medwatch or 1-800-FDA-1088.

Common Side Effects

Common side effects of Xeljanz include infections and cold-like symptoms, such as congestion, runny nose, and sore throat.

Less common side effects may include:

  • Headache 
  • Rash
  • Gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea) 
  • High blood pressure
  • Increased cholesterol levels

Severe Side Effects

Remember that Xeljanz works by interfering with messaging between immune system cells. As a result, this medication can increase your susceptibility to infections such as tuberculosis. Infections may be severe and result in hospitalizations or death.

For this reason, your healthcare providers will carefully monitor you for signs of an infection while on Xeljanz. In particular, treatment with Xeljanz may cause reactivation of dormant hepatitis infection. Tell your healthcare team if you may have chronic hepatitis or any other infection before starting treatment with Xeljanz.

Additionally, Xeljanx may increase the risk of:

  • Certain cancers, especially cancers of the immune system (e.g., lymphoma)
  • Blood clots in leg veins (deep venous thrombosis, or DVT), lungs (pulmonary embolism, or PE), or arteries
  • All-cause or heart-related death in people older than 50 years with one or more risk factors for heart disease (e.g., heart attack, peripheral vascular disease, or stroke)

Healthcare providers usually avoid prescribing Xeljanz for people with a history of blood clots. Other potential risk factors include heart failure, inherited blood clotting disorders, cancer, and planning to have or have had recent major surgery.

Other serious side effects can include:

  • Tears in your digestive system in the form of stomach ulcers or diverticulitis of the colon
  • Changes in blood counts (like white and red blood cells): These may need to be monitored while you are on therapy.
  • Changes in liver enzymes in the blood, which may also need to be monitored.

Dosage: How Much of Xeljanz Should I Take?

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The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For psoriatic arthritis and rheumatoid arthritis:
    • For oral dosage form (extended-release tablets):
      • Adults—11 milligrams (mg) once a day together with another medicine. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For oral dosage form (tablets):
      • Adults—5 milligrams (mg) 2 times a day together with another medicine. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
  • For ulcerative colitis:
    • For oral dosage form (extended-release tablets):
      • Adults—22 milligrams (mg) once a day for at least 8 weeks, then 11 mg once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For oral dosage form (tablets):
      • Adults—10 milligrams (mg) 2 times a day for at least 8 weeks, then 5 or 10 mg 2 times a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
  • For pcJIA:
    • For oral dosage form (tablets):
      • Children 2 to 17 years of age—Dose is based on body weight and must be determined by your doctor.
        • Weighing 40 kilograms (kg) or more—5 milligrams (mg) 2 times a day. Your doctor may adjust your dose as needed.
        • Weighing 20 to less than 40 kg—4 mg 2 times a day. Your doctor may adjust your dose as needed.
        • Weighing 10 to less than 20 kg—3.2 mg 2 times a day. Your doctor may adjust your dose as needed.
      • Children younger than 2 years of age—Use and dose must be determined by your doctor.
    • For oral dosage form (solution):
      • Children 2 to 17 years of age—Dose is based on body weight and must be determined by your doctor.
        • Weighing 40 kilograms (kg) or more—5 milliliters (mL) 2 times a day. Your doctor may adjust your dose as needed.
        • Weighing 20 to less than 40 kg—4 mL 2 times a day. Your doctor may adjust your dose as needed.
        • Weighing 10 to less than 20 kg—3.2 mL 2 times a day. Your doctor may adjust your dose as needed.
      • Children younger than 2 years of age—Use and dose must be determined by your doctor.

Modifications

Your healthcare provider may adjust your dose of Xeljanz if you have kidney disease or moderate liver disease. It is generally not recommended for people with severe liver disease to take Xeljanz. It is unknown if Xeljanz is safe to use if you have hepatitis B or hepatitis C.

Missed Dose

If you miss a dose of Xeljanz, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double up on doses.

Overdose: What Happens if I Use Too Much Xeljanz?

Immediately call your healthcare provider if you accidentally take too much Xeljanz. Your healthcare provider may monitor you for signs of adverse reactions.

What Happens If I Overdose on Xeljanz?

Xeljanz may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your healthcare provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Precautions

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It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if this medicine is working properly and to decide whether you should continue to use it. Blood tests are needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using this medicine, tell your doctor right away.

If you plan to have children, talk with your doctor before using this medicine. Some women using this medicine have become infertile (unable to have children).

You will need to have a skin test for tuberculosis before you start using this medicine. Tell your doctor if you or anyone in your home has ever had a positive reaction to a tuberculosis skin test.

This medicine may increase your risk of serious heart or blood vessel problems (eg, heart attack, stroke), especially in patients with rheumatoid arthritis who are 50 years of age and older and with a heart or blood vessel disease. Call your doctor right away if you have chest pain or discomfort, confusion, difficulty in speaking, double vision, headache, inability to move arms, legs, or facial muscles, nausea, pain or discomfort in the arms, jaw, back, or neck, sweating, trouble breathing, or vomiting.

Your body's ability to fight infections may be reduced while you are using tofacitinib. It is very important that you call your doctor at the first sign of an infection. Check with your doctor right away if you have a fever, chills, cough, flu-like symptoms, or unusual tiredness or weakness.

This medicine may increase your risk of cancer (eg, lymphoma, lung cancer, non-melanoma skin cancer). Tell your doctor right away if you have black, tarry stools, general feeling of illness, swollen glands, weight loss, yellow skin and eyes, persistent non-healing sore, reddish patch or irritated area, shiny bump, pink growth, or white, yellow or waxy scar-like area on the skin.

This medicine can cause serious allergic reactions, including angioedema or urticaria. Tell your doctor right away if you start to have swelling of your face, lips, tongue, throat, arms, or legs, or if you are having trouble swallowing or breathing.

Tofacitinib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection:

  • If you can, avoid people with infections. Check with your doctor right away if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
  • Check with your doctor right away if you notice any unusual bleeding or bruising, black, tarry stools, blood in the urine or stools, or pinpoint red spots on your skin.
  • Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
  • Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
  • Be careful not to cut yourself when you are using sharp objects, such as a safety razor or fingernail or toenail cutters.
  • Avoid contact sports or other situations where bruising or injury could occur.

This medicine may increase your risk of developing blood clots (eg, arterial thrombosis, deep vein thrombosis, pulmonary embolism), especially in patients with rheumatoid arthritis who are 50 years of age and older and with a heart or blood vessel disease. Check with your doctor right away if you have anxiety, chest pain, cough, dizziness, lightheadedness, or fainting, fast heartbeat, pain, redness, or swelling in the arm or leg, pains in the chest, groin, or legs, especially calves of the legs, severe headaches, sudden loss of coordination, sudden onset of slurred speech, sudden vision changes, or trouble breathing.

While you are being treated with tofacitinib, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Tofacitinib may lower your body's resistance and there is a chance you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

What Are Reasons I Shouldn’t Take Xeljanz?

You may not be able to take Xeljanz if you:

  • Are allergic to Xeljanz or any of its ingredients
  • Develop a serious infection, or your white blood cell count drops too low
  • Have severe liver disease or a history of hepatitis B or C
  • Are pregnant: Limited information exists on whether Xeljanz is safe to use during pregnancy. Your healthcare provider may decide not to prescribe it to you while pregnant, especially in the first trimester.
  • Are breastfeeding: It is unknown if Xeljanz passes into human breast milk. After stopping the medication, wait at least 18 hours before breastfeeding and at least 36 hours if you take the extended-release formulation.

What Other Medications Interact With Xeljanz?

Drug interactions can occur when taking Xeljanz with certain medications. Make sure your healthcare team is aware of all medications, herbs, and supplements you take before starting therapy.

Taking other drugs that suppress the immune system (i.e., immunosuppressants) with Xeljanz can increase your risk of infection. Examples of immunosuppressants include:

  • Azasan, Imuran (azathioprine)
  • Astagraf XL, Envarsus XR, Prograf, Protopic (tacrolimus)
  • Gengraf, Neoral, Sandimmune (cyclosporine)

Xeljanz is processed in the body by a set of enzymes called cytochrome P450 3A4 (CYP3A4). Some drugs can decrease or increase the activity of these enzymes, causing an unpredictable increase or decrease in levels of tofacitinib, respectively. As such, Xeljanz can interact with:

Since Xeljanz affects the immune system, let your healthcare provider know if you plan to get any vaccines. People on Xeljanz should not get live vaccines, though non-live vaccines are OK.

Live vaccines include:

  • Measles, mumps, rubella (MMR) vaccine
  • Rotavirus vaccine
  • Smallpox vaccine
  • Chickenpox vaccine
  • Yellow fever vaccine

Xeljanz treatment may also affect how well the COVID-19 vaccines work. Your therapy may need to be adjusted accordingly.

What Medications Are Similar?

There are many types of immunosuppressants available to treat autoimmune diseases. Immunosuppressant drugs that use molecular biology to target individual molecules in the immune system are sometimes called “biologic agents,” “targeted biologic agents,” or “biologics.” These include drugs like Humira (adalimumab) which targets tumor necrosis factor to treat RA or Rituxan (rituximab), which targets CD20 to treat lymphoma.

 Xeljanz is considered a non-biologic agent that targets JAK molecules. The other available JAK inhibitor is Jakafi (ruxolitinib), which treats myelofibrosis (a disease of the bone marrow).

Frequently Asked Questions

  • What is Xeljanz used for?

    Xeljanz is approved to treat certain types of inflammatory and autoimmune conditions, such as rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular course juvenile idiopathic arthritis.

  • How does Xeljanz work?

    Xeljanz interferes with signals sent between cells in the immune system to treat inflammatory and autoimmune diseases.

  • What are the most common side effects of Xeljanz?

    Common side effects of Xeljanz include infections and cold-like symptoms. People sometimes also experience headaches, rash, and gastrointestinal symptoms such as nausea, vomiting, and diarrhea. High blood pressure and increased cholesterol levels have also been seen.

  • Are there any serious side effects associated with Xeljanz?

    Some serious side effects have been reported with Xeljanz therapy. These include an increased risk of serious infections, some types of cancer, and blood clots. Older people with rheumatoid arthritis with at least one risk factor for heart disease may have an increased risk of death from all causes. For this reason, higher doses of Xeljanz are not recommended for people with rheumatoid or psoriatic arthritis.

How Can I Stay Healthy While Taking Xeljanz?

Chronic autoimmune conditions such as PsA, RA, and ulcerative colitis can be mentally and physically debilitating. Fortunately, scientists are developing drugs to target the individual molecules that play a role in causing these diseases. There are more treatment options than ever before, and drugs like Xeljanz offer hope to people who have not responded well to other medications.

It is important to remember that this medication can affect your immune system's ability to fight infections. Tell your healthcare provider right away if you develop any signs of an infection. Try to reduce your risk of infection by avoiding close contact with other people who are sick and maintaining good hygiene practices.

You should also discuss vaccinations with your healthcare team. You might need to wait to start Xeljanz until you are up to date on certain immunizations. This is because Xeljanz can affect how certain vaccines work. Non-live vaccines, such as your annual flu shot and pneumococcal vaccines, are OK to receive during treatment.

Medical Disclaimer

Verywell Health's drug information is meant for educational purposes only and is not intended to replace medical advice, diagnosis, or treatment from a healthcare provider. Consult your healthcare provider before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

10 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
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By Rony Kampalath, MD
Rony Kampalath, MD, is board-certified in diagnostic radiology and previously worked as a primary care physician. He is an assistant professor at the University of California at Irvine Medical Center, where he also practices. Within the practice of radiology, he specializes in abdominal imaging.