Xeljanz and Xeljanz XR are brand-name prescription medications.

They are FDA-approved for use in certain adults with:

Xeljanz is also FDA-approved for use in certain children ages 2 years and older with polyarticular juvenile idiopathic arthritis.

Xeljanz and Xeljanz XR are used to treat these conditions in people who’ve tried certain other drugs that either weren’t effective enough for them or caused bothersome side effects. Xeljanz and Xeljanz XR also have certain limitations.

To read more about these uses and the drugs’ limitations, see the “Xeljanz uses” section below.

Xeljanz and Xeljanz XR

Xeljanz is available in these forms:

  • Xeljanz (immediate release), which is released at once in your body after it’s taken. It comes as:
    • 5-milligram (mg) and 10-mg oral tablets
    • 1 mg/milliliter oral solution
  • Xeljanz XR (extended release), which is released slowly over time in your body after it’s taken. It comes as:
    • 11-mg and 22-mg oral tablets

Drug details

Xeljanz contains the drug tofacitinib. It belongs to a class of drugs called Janus kinase inhibitors. These drugs help to decrease inflammation in your body.

Xeljanz comes as a tablet and solution that’s taken by mouth. You’ll take it either once or twice a day, depending on the form of the drug your doctor prescribes.

Effectiveness

Xeljanz and Xeljanz XR have been found effective in clinical trials to treat the conditions listed above. See the “Xeljanz uses” section below for details about the drugs’ effectiveness.

Xeljanz is available only as a brand-name medication. It’s not currently available in generic form.

Xeljanz contains the active drug tofacitinib.

Xeljanz and Xeljanz XR can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking either drug. These lists do not include all possible side effects.

For more information on the possible side effects of Xeljanz and Xeljanz XR, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome.

More common side effects

The more common side effects of Xeljanz and Xeljanz XR can include:

Most of these side effects may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk with your doctor or pharmacist.

* For more information about this side effect, see “Side effect details” below.

Serious side effects

Serious side effects from Xeljanz and Xeljanz XR aren’t common, but they can occur. Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life threatening or if you think you’re having a medical emergency.

Serious side effects and their symptoms can include the following:

  • Gastrointestinal perforations (tears in your digestive tract). Symptoms can include:
    • fever
    • pain in your belly or stomach area
    • changes in your bowel movements, such as having diarrhea or constipation
  • Blood disorders, including low levels of red blood cells and white blood cells (such as neutrophils and lymphocytes). Symptoms can include:
    • frequent infections
    • fever
    • fatigue (lack of energy)
    • weakness
    • shortness of breath
  • Cardiovascular problems, such as heart attack or stroke, which may be more likely in people with certain risk factors. Symptoms can include:
    • chest pain
    • shortness of breath
    • feeling lightheaded
    • sudden weakness on one side of your body
    • slurred speech
  • Risk of serious infections.* These include reactivation (flare-up) of infections you may already have, such as tuberculosis (TB), hepatitis B or C, or herpes zoster (shingles). The most common infections seen in clinical studies were pneumonia, skin infection, and urinary tract infection (UTI). Your symptoms will depend on the type of infection you have, but they can include:
    • fever
    • fatigue
    • muscle aches
    • chills
    • rash
    • cough
    • unexplained weight loss
  • Risk of blood clots in your legs or arms. These clots can move to your lungs and block blood flow, which prevents oxygen from traveling through your body.* Symptoms of blood clots can include:
    • shortness of breath
    • chest pain
    • swelling in your arm or leg
    • pain in your arm or leg
    • trouble breathing
  • Risk of cancer, including skin cancer and lymphoma (a type of blood cancer).* Symptoms can include:
    • changes in moles on your skin
    • fatigue
    • unexplained weight loss
    • frequent infections
  • Risk of death in certain people.*
  • Allergic reaction.†

* Xeljanz has boxed warnings from the FDA regarding the risk of this side effect. A boxed warning is the strongest warning the FDA requires. It alerts doctors and patients about drug effects that may be dangerous. See the “FDA warnings” section at the beginning of this article to learn more.
† For more information about this side effect, see “Side effect details” below.

Side effect details

You may wonder how often certain side effects occur with this drug, or whether certain side effects pertain to it. Here’s some detail on some of the side effects this drug may or may not cause.

Allergic reaction

As with most drugs, some people can have an allergic reaction after taking Xeljanz or Xeljanz XR. It’s not known how often allergic reactions occur with either drug.

Symptoms of a mild allergic reaction can include:

A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:

  • swelling under your skin, typically in your eyelids, lips, hands, or feet
  • swelling of your tongue, mouth, or throat
  • trouble breathing

Call your doctor right away if you have a severe allergic reaction to Xeljanz or Xeljanz XR. Call 911 if your symptoms feel life threatening or if you think you’re having a medical emergency.

Rash

A rash is a possible side effect of Xeljanz and Xeljanz XR. During clinical studies, a rash was one of the more common side effects.

In clinical studies, up to 6% of people who took Xeljanz had a rash. Of people taking a placebo (treatment with no active drug), 4% had a rash. The same side effects and frequencies are expected with Xeljanz XR.

Rash may also be a sign of a more serious side effect, such as herpes zoster (shingles). This is an infection caused by the chickenpox virus. If you’ve had chickenpox in the past, the virus usually lies dormant (inactive) inside your body. However, sometimes the virus flares up, resulting in shingles.

Unlike an allergic reaction to a drug, which can cause an itchy rash, shingles typically causes tingling and pain over an area of your skin. This is followed by a blistering rash that often requires medical treatment.

If you have a rash while you’re taking Xeljanz or Xeljanz XR, talk with your doctor. They’ll check to see what’s causing it, and they’ll recommend whether any treatment is needed.

Headache

You may have headaches while you’re taking Xeljanz or Xeljanz XR. This was one of the more common side effects that occurred in clinical studies.

During studies, up to 9% of people taking Xeljanz had headaches. Of people taking a placebo (treatment with no active drug), up to 6% had headaches. The same side effects and frequencies are expected with Xeljanz XR.

If you have headaches while you’re taking Xeljanz or Xeljanz XR, talk with your doctor. They can recommend safe and effective treatment options for your discomfort.

Skin side effects

Skin side effects may occur during treatment with Xeljanz or Xeljanz XR. These side effects include rash (see “Rash” above), skin discoloration, itchiness, and acne.

In clinical studies of Xeljanz in people with ulcerative colitis (UC), at least 2% of people who took the drug had acne as a side effect. Acne was seen in at least 1% more people taking Xeljanz than in people taking a placebo (treatment with no active drug). The same side effects and frequencies are expected with Xeljanz XR.

More serious skin conditions that may be caused by Xeljanz or Xeljanz XR include skin cancers, such as nonmelanoma skin cancer.* A higher risk of skin cancer was seen in people taking higher dosages (10 milligrams [mg] twice a day) of Xeljanz, compared to those taking lower dosages. (Note that 10 mg of Xeljanz twice a day is equivalent to 22 mg of Xeljanz XR once a day.)

Tell your doctor if you have any skin side effects, including changes in moles or beauty marks, while you’re taking Xeljanz. Your doctor will recommend whether you need treatment for these side effects.

* Xeljanz has a boxed warning for cancers, including nonmelanoma skin cancer. A boxed warning is the strongest warning the FDA requires. It alerts doctors and patients about drug effects that may be dangerous. See the “FDA warnings” section at the beginning of this article to learn more.

Fatigue

Fatigue is a possible side effect of Xeljanz and Xeljanz XR. However, it’s not known how often this side effect occurred in clinical studies.

Fatigue may also be a symptom of more serious side effects of Xeljanz and Xeljanz XR, including:

  • serious infections*
  • blood disorders, such as anemia (low red blood cell level)
  • cancer*

If you have fatigue while you’re taking Xeljanz or Xeljanz XR, tell your doctor. They may check to see what’s causing your fatigue, and they’ll recommend ways to improve your energy levels.

* Xeljanz has a boxed warning for this side effect. A boxed warning is the strongest warning the FDA requires. It alerts doctors and patients about drug effects that may be dangerous. See the “FDA warnings” section at the beginning of this article to learn more.

Increased cholesterol

Increased cholesterol levels may occur while you take Xeljanz or Xeljanz XR. In clinical studies, after 1 month of treatment, people who took Xeljanz had increased levels of both:

  • low-density lipoprotein (LDL), which is also called “bad” cholesterol, and
  • high-density lipoprotein (HDL), which is also called “good” cholesterol

In clinical studies of people with rheumatoid arthritis (RA), 15% to 19% of people who took Xeljanz had increased LDL levels during the first 3 months of treatment. Between 10% and 12% of people taking Xeljanz had increased HDL levels during this same period of time.

In studies of people with psoriatic arthritis (PsA) who took Xeljanz, similar numbers of people had increased cholesterol levels.

In clinical studies of people with ulcerative colitis (UC), 5% to 9% of people who took Xeljanz had increased cholesterol levels during treatment. Of people who took a placebo (treatment with no active drug), 1% had the same result.

The same side effects and frequencies are expected with Xeljanz XR.

During Xeljanz or Xeljanz XR treatment, your doctor will check your cholesterol levels about 1 to 2 months after you’ve started taking the drug. If your cholesterol levels are too high, your doctor will likely prescribe medication to help lower the level.

Weight gain or weight loss (not a side effect)

Weight gain and weight loss haven’t been reported with Xeljanz or Xeljanz XR. These side effects weren’t seen during clinical studies.

However, Xeljanz and Xeljanz XR can increase your risk for serious infections, such as tuberculosis (TB). With TB, some people can have weight loss.

If you have unexplained weight loss while you’re taking either drug, tell your doctor. They may check to see what’s causing your weight loss, and they’ll recommend whether or not you need medical treatment.

Hair loss (not a side effect)

Hair loss isn’t a side effect of Xeljanz or Xeljanz XR. In fact, tofacitinib (the active drug in Xeljanz) has been tested in several small studies, including this one from 2017 and this one from 2018, as a treatment for hair loss. For more details about this use, see the section “Xeljanz for other conditions” below.

The Food and Drug Administration (FDA) approves prescription drugs such as Xeljanz and Xeljanz XR to treat certain conditions. Either drug may also be prescribed off-label for other conditions. Off-label use is when a drug that’s approved to treat one condition is used to treat a different condition.

Xeljanz for ulcerative colitis

Xeljanz and Xeljanz XR are FDA-approved to treat moderately to severely active ulcerative colitis (UC) in adults. Either drug is used for people who didn’t receive enough benefit from other medications called tumor necrosis factor (TNF) inhibitors. Either is also used in people who had bothersome side effects from TNF inhibitors.

With UC, the lining inside of your colon (large intestine) or rectum is inflamed. This long-term condition can cause abdominal pain, diarrhea, and blood in your stools.

Xeljanz and Xeljanz XR should not be used in combination with certain other drugs for UC.Examples of these drugs include infliximab (Remicade), azathioprine (Imuran), and cyclosporine (Neoral).

Effectiveness for ulcerative colitis

Tofacitinib (the active drug in Xeljanz and Xeljanz XR) has been found to be effective in treating UC. It’s recommended in treatment guidelines from the American College of Gastroenterology. For information about how the drug performed in clinical trials, see the prescribing information.

Xeljanz for rheumatoid arthritis

Xeljanz and Xeljanz XR are FDA-approved to treat moderately or severely active rheumatoid arthritis (RA) in adults. Either drug is used for people who didn’t receive enough benefit from other medications called tumor necrosis factor (TNF) inhibitors. Either is also used in people who had bothersome side effects of TNF inhibitors.

RA is an autoimmune condition that causes pain and swelling in your joints. Over time, it can cause damage to your joints.

Xeljanz and Xeljanz XR should not be used in combination with certain other drugs for RA.Examples of these drugs include infliximab (Remicade), azathioprine (Imuran), and cyclosporine (Neoral).

Effectiveness for rheumatoid arthritis

Tofacitinib (the active drug in Xeljanz and Xeljanz XR) has been found to be effective in treating RA. It’s recommended in treatment guidelines from the American College of Rheumatology. For information about how the drug performed in clinical trials, see the prescribing information.

Xeljanz for psoriatic arthritis

Xeljanz and Xeljanz XR are FDA-approved to treat active psoriatic arthritis (PsA) in adults. Either drug is used for people who didn’t receive enough benefit from other medications called tumor necrosis factor (TNF) inhibitors. Either is also used in people who had bothersome side effects of TNF inhibitors.

With PsA, people have symptoms of arthritis (such as sore, swollen joints) and symptoms of psoriasis (such as red, scaly patches on your skin). This is a long-term autoimmune condition.

Xeljanz and Xeljanz XR should not be used in combination with certain other drugs for PsA.

Effectiveness for psoriatic arthritis

Tofacitinib (the active drug in Xeljanz and Xeljanz XR) has been found to be effective in treating PsA. It’s recommended in treatment guidelines from the American College of Rheumatology. For information about how the drug performed in clinical trials, see the prescribing information.

Xeljanz for ankylosing spondylitis

Xeljanz and Xeljanz XR are FDA-approved to treat active ankylosing spondylitis (AS) in adults. Either drug is used for people who didn’t receive enough benefit from other medications called tumor necrosis factor (TNF) inhibitors. Either is also used in people who had bothersome side effects of TNF inhibitors.

Xeljanz and Xeljanz XR should not be used in combination with certain other drugs for AS.

With AS, the ligaments and tendons that attach to your spine are inflamed. This form of arthritis can cause pain and stiffness in your spine and back.

Effectiveness for ankylosing spondylitis

Tofacitinib (the active drug in Xeljanz and Xeljanz XR) has been found to be effective in treating AS. It’s included as a treatment option in guidelines from the American College of Rheumatology. For information about how the drug performed in clinical trials, see the prescribing information.

Xeljanz and children

Xeljanz is FDA-approved for use in certain children ages 2 years and older who have polyarticular juvenile idiopathic arthritis (JIA).

This drug is used for children who didn’t receive enough benefit from other medications called tumor necrosis factor (TNF) inhibitors. Xeljanz is also used for children who had bothersome side effects of TNF inhibitors.

The drug should not be used in combination with certain other medications for JIA.

This is a form of arthritis in children that affects several joints. It can cause joint pain and stiffness, as well a rash, a fever, and fatigue.

Effectiveness in children with juvenile idiopathic arthritis

Xeljanz has been found to be effective in treating JIA. For information about how the drug performed in clinical trials, see the prescribing information.

Xeljanz for other conditions

In addition to the uses listed above, Xeljanz and Xeljanz XR may be used off-label. Off-label drug use is when a drug that’s approved for one use is prescribed for a different one that’s not approved. You may wonder if Xeljanz or Xeljanz XR is used for certain other conditions.

Xeljanz for alopecia (off-label use)

Xeljanz and Xeljanz XR aren’t approved to treat alopecia (hair loss), but sometimes they’re prescribed off-label for this condition. A review of several small clinical studies found that tofacitinib (the active drug in Xeljanz and Xeljanz XR) may be effective to treat alopecia. However, more studies are needed to fully understand the role of these drugs in treating hair loss.

If you’d like to know more about treatment options for hair loss, talk with your doctor.

Xeljanz for psoriasis (off-label use)

Xeljanz and Xeljanz XR aren’t approved to treat psoriasis, but sometimes they’re prescribed off-label for this condition. However, Xeljanz and Xeljanz XR are approved to treat psoriatic arthritis (PsA), which is closely related to psoriasis.

In a pooled analysis of six clinical studies, tofacitinib (the active drug in Xeljanz and Xeljanz XR) was found to be more effective than a placebo (no active drug) in treating plaque psoriasis.

If you’d like to know more about treatment options for psoriasis, talk with your doctor.

Xeljanz for vitiligo (off-label use)

Xeljanz and Xeljanz XR aren’t approved to treat vitiligo, which is condition where your skin loses pigmentation (color) in some areas. However, both drugs are sometimes prescribed off-label for this condition.

One review looked at several small clinical studies and case reports that included tofacitinib (the active drug in Xeljanz and Xeljanz XR) as a treatment for vitiligo. This drug was found to help produce pigmentation (skin color) in some people. In particular, tofacitinib was found to cause repigmentation (return of skin color) when it was used in combination with light therapy.

If you’d like to know more about treatment options for vitiligo, talk with your doctor.

Xeljanz for lupus (off-label use)

Xeljanz and Xeljanz XR aren’t approved to treat lupus, but sometimes they’re prescribed off-label for this purpose.

A small clinical study found that tofacitinib (the active drug in Xeljanz and Xeljanz XR) improved skin rash and joint pain in people with systemic lupus erythematosus (SLE).

If you’d like to know more about treatment options for lupus, talk with your doctor.

Xeljanz for eczema (off-label use)

Xeljanz and Xeljanz XR aren’t approved for treating eczema, but sometimes they’re prescribed off-label for this condition.

One small clinical study looked at using tofacitinib (the active drug in Xeljanz and Xeljanz XR) topically on people’s skin, rather than having them take the drug by mouth. In this study, people’s eczema symptoms were reduced more with tofacitinib than with a topical placebo (no active drug).

If you’d like to know more about treatment options for eczema, talk with your doctor.

The Xeljanz or Xeljanz XR dosage your doctor prescribes will depend on several factors. These include:

  • the condition you’re using the drug to treat
  • how your body responds to the drug
  • the form of Xeljanz you’re taking
  • other medical conditions that you may have
  • other medications that you may be taking

Typically, your doctor will start you on a low dosage. Then they’ll adjust it over time to reach the amount that’s right for you. Your doctor will ultimately prescribe the smallest dosage that provides the desired effect.

The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to suit your needs.

Drug forms and strengths

Xeljanz comes in two forms, which are each taken by mouth. The forms are:

  • Xeljanz (immediate release), which is released at once in your body after it’s taken. It comes as:
    • 5-milligram (mg) and 10-mg oral tablets
    • 1 mg/milliliter (mL) oral solution
  • Xeljanz XR (extended release), which is released slowly over time in your body after it’s taken. It comes as:
    • 11-mg and 22-mg oral tablets

Dosage for ulcerative colitis

The usual dosages of Xeljanz and Xeljanz XR for ulcerative colitis (UC) depend on the specific purpose of the treatment.

Both can be used to induce (cause) or maintain (keep) remission of UC. Remission is generally described as having very few or no UC symptoms.

Dosage to induce remission of ulcerative colitis

To induce UC remission, the typical dosage of Xeljanz is 10 mg twice each day for 8 weeks. Xeljanz XR has a dosage of 22 mg once daily for 8 weeks.

If your UC is in remission after 8 weeks, your doctor will prescribe the maintenance dosage of Xeljanz or Xeljanz XR for you to take going forward. If your UC isn’t in remission after 8 weeks, your doctor may have you take the induction dosage of Xeljanz or Xeljanz XR for up to 16 weeks.

Dosage to maintain remission of ulcerative colitis

To maintain UC remission, the usual dosage of Xeljanz is 5 mg twice a day. Xeljanz XR has a dosage of 11 mg once daily.

Dosage for rheumatoid arthritis

The usual dosage for rheumatoid arthritis (RA) in each form of Xeljanz is as follows:

  • Xeljanz 5 mg taken by mouth twice each day
  • Xeljanz XR 11 mg taken by mouth once a day

Dosage for psoriatic arthritis

The usual dosage for psoriatic arthritis (PsA) in each form of Xeljanz is as follows:

  • Xeljanz 5 mg taken by mouth twice each day
  • Xeljanz XR 11 mg taken by mouth once a day

Dosage for ankylosing spondylitis

The usual dosage for ankylosing spondylitis (AS) in each form of Xeljanz is as follows :

  • Xeljanz: 5 mg taken by mouth twice a day
  • Xeljanz XR: 11 mg taken by mouth once a day

Children’s dosage

The usual dosage of Xeljanz oral solution and oral tablets for children to treat juvenile idiopathic arthritis is based on body weight in kilograms (kg). One kilogram is equal to about 2.2 pounds (lb).

Recommended dosages are as follows:

  • for children weighing 10 kg (about 22 lb) to less than 20 kg (about 44 lb), their dosage will be 3.2 mg twice daily. This is equal to 3.2 mL of Xeljanz oral solution.
  • for children weighing 20 kg to less than 40 kg (about 88 lb), their dosage will be 4 mg twice daily. This is equal to 4 mL of Xeljanz oral solution.
  • for children weighing more than 40 kg, their dosage will be 5 mg twice daily. This is equal to 5 mL of Xeljanz oral solution. Alternately, children with this body weight may take Xeljanz 5-mg oral tablets rather than the oral solution.

What if I miss a dose?

If you miss a dose of Xeljanz or Xeljanz XR, let your healthcare professional know. They’ll recommend whether you should take the missed dose or wait until your next regular dose. Don’t take more than one dose of Xeljanz or Xeljanz XR at a time. This can lead to serious side effects.

To help make sure that you don’t miss a dose, try setting a reminder on your phone. A medication timer may be useful, too.

Will I need to use this drug long term?

Xeljanz and Xeljanz XR are meant to be used as a long-term treatment. If you and your doctor determine that either drug is safe and effective for you, you’ll likely take it long term.

There aren’t any known interactions between Xeljanz or Xeljanz XR and alcohol. If you drink alcohol, ask your doctor whether it’s safe to drink it during treatment with either medication.

Xeljanz and Xeljanz XR can interact with several other medications. These drugs can also interact with certain supplements as well as certain foods.

Different interactions can cause different effects. For instance, some interactions can interfere with how well a drug works. Other interactions can increase side effects or make them more severe.

Xeljanz and other medications

Below are lists of medications that can interact with Xeljanz and Xeljanz XR. These lists do not contain all the drugs that may interact with the medications.

Before taking Xeljanz or Xeljanz XR, talk with your doctor and pharmacist. Tell them about all prescription, over-the-counter, and other drugs you take. Also tell them about any vitamins, herbs, and supplements you use. Sharing this information can help you avoid potential interactions.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Xeljanz and certain antibiotics and antifungals

Taking Xeljanz or Xeljanz XR with certain antibiotics and antifungals can increase your risk of serious side effects. Certain antibiotics and antifungals can prevent your body from breaking down Xeljanz and Xeljanz XR. This leads to high levels of Xeljanz or Xeljanz XR in your body, which can increase side effects from the drug.

Examples of antibiotics that can increase your risk of serious side effects if taken with Xeljanz or Xeljanz XR include:

  • clarithromycin (Biaxin XL)
  • erythromycin (Ery-Tab, Eryped, many others)

Examples of antifungals that can increase your risk of serious side effects if taken with Xeljanz or Xeljanz XR include:

  • ketoconazole (Extina, Nizoral, Xolegel)
  • fluconazole (Diflucan)
  • itraconazole (Omnel, Sporanox, Tolsura)
  • voriconazole (Vfend)

If you need to take one of these antibiotics or antifungals while you’re taking Xeljanz or Xeljanz XR, your doctor will monitor you closely for side effects. Your doctor will also likely recommend that you take a lower dosage of Xeljanz or Xeljanz XR until you’re no longer taking the antibiotic or antifungal.

Xeljanz and certain seizure drugs

Taking Xeljanz or Xeljanz XR with certain seizure medications can increase how quickly your body clears Xeljanz or Xeljanz XR. This lowers your levels of these drugs, which could decrease their effectiveness to treat your condition.

Examples of seizure drugs that can decrease the effectiveness of Xeljanz or Xeljanz XR include:

  • carbamazepine (Carbatrol, Epitol, Equetro, Tegretol)
  • phenytoin (Dilantin, Phenytek)
  • phenobarbital

If you need to take a seizure medication with Xeljanz or Xeljanz XR, your doctor may change your seizure medication, or they may prescribe a drug other than Xeljanz or Xeljanz XR for you.

Xeljanz and certain drugs that suppress your immune system

Taking Xeljanz with certain drugs that suppress (decrease the ability of) your immune system can increase your risk of serious infections.

Examples of drugs that can increase your risk of serious infections if taken with Xeljanz or Xeljanz XR include:

Taking Xeljanz or Xeljanz XR with these drugs isn’t recommended. Be sure to tell your doctor about all medications you’re taking before you start Xeljanz or Xeljanz XR.

Xeljanz and herbs and supplements

There aren’t any herbs or supplements that have been specifically reported to interact with Xeljanz and Xeljanz XR. However, you should still check with your doctor or pharmacist before using any of these products while taking either drug.

Xeljanz and foods

Eating grapefruit or drinking grapefruit juice while you’re taking Xeljanz or Xeljanz XR could increase your risk of serious side effects. This is because grapefruit prevents your body from breaking down and clearing Xeljanz or Xeljanz XR. This leads to higher levels of the drug in your body.

Talk with your doctor about how much grapefruit is safe for you to consume while you’re taking Xeljanz or Xeljanz XR.

Other drugs are available that can treat your condition. Some may be better suited for you than others. If you’re interested in finding an alternative to Xeljanz or Xeljanz XR, talk with your doctor. They can tell you about other medications that may work well for you.

Note: Some of the drugs listed here are used off-label to treat these specific conditions. Off-label use is when a drug that’s approved to treat one condition is used to treat a different condition.

Alternatives for ulcerative colitis

Examples of other drugs that may be used to treat ulcerative colitis (UC) include:

  • mesalamine (Apriso, Asacol HD, Canasa, Lialda)
  • olsalazine (Dipentum)
  • sulfasalazine (Azulfidine)
  • budesonide (Uceris)
  • azathioprine (Azasan, Imuran)
  • mercaptopurine (Purinethol, Purixan)
  • adalimumab (Amjevita, Cyltezo, Hadlima, Humira, Hyrimoz)
  • golimumab (Simponi)
  • infliximab (Inflectra, Ixifi, Remicade, Renflexis)
  • vedolizumab (Entyvio)

Alternatives for rheumatoid arthritis

Examples of other drugs that may be used to treat rheumatoid arthritis (RA) include:

Alternatives for psoriatic arthritis

Examples of other drugs that may be used to treat psoriatic arthritis (PsA) include:

Alternatives for ankylosing spondylitis

Examples of other drugs that may be used to treat ankylosing spondylitis (AS) include:

Alternatives for juvenile idiopathic arthritis

Examples of other drugs that may be used to treat juvenile idiopathic arthritis (JIA)include:

Xeljanz, Xeljanz XR, and Rinvoq are used for similar purposes. In fact, they’re all approved to treat the following conditions in adults:

Additionally, Rinvoq treats atopic dermatitis (also called eczema) in certain people ages 12 years and older. And Xeljanz treats juvenile idiopathic arthritis in children and adults ages 2 years and older.

These medications each come as oral tablets. Additionally, Xeljanz comes as an oral solution.

To learn more about the similarities and differences of treatment with Rinvoq, see this detailed comparison. Also, talk with your doctor about which treatment may be right for your condition.

You may wonder how Xeljanz compares to other medications that are prescribed for similar uses. Here we look at how Xeljanz and Humira are alike and different.

Uses

Xeljanz and Humira are both approved for use in adults with:

They’re also both used for juvenile idiopathic arthritis in children and adults ages 2 years and older.

Humira is also approved to treat:

Drug forms and administration

Xeljanz contains the drug tofacitinib. It comes as a tablet that’s taken by mouth, once or twice a day. It also comes as an oral solution that’s taken twice daily.

Humira contains the drug adalimumab. It’s given as a subcutaneous injection, typically once every other week. Your healthcare professional may give you the injection, or they may show you how to self-inject Humira at home.

Side effects and risks

Xeljanz and Humira contain different drugs. Therefore, they can cause some similar side effects and some different side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Xeljanz, with Humira, or with both drugs (when taken individually).

  • Can occur with Xeljanz:
  • Can occur with Humira:
    • injection site reactions
    • abdominal pain
  • Can occur with both Xeljanz and Humira:
    • headache
    • upper respiratory infections, such as the common cold
    • rash

Serious side effects

These lists contain examples of serious side effects that can occur with Xeljanz, with Humira, or with both drugs (when taken individually).

* Xeljanz and Humira both have boxed warnings from the FDA regarding the risk of serious infections and cancer. Xeljanz also has a boxed warning regarding the risk of blood clots and increased risk of death. A boxed warning is the strongest warning the FDA requires. It alerts doctors and patients about drug effects that may be dangerous.

Effectiveness

Xeljanz and Humira have different FDA-approved uses, but they’re both used to treat the following conditions:

  • ulcerative colitis (UC)
  • rheumatoid arthritis (RA)
  • psoriatic arthritis (PsA)
  • ankylosing spondylitis (AS)

These drugs haven’t been directly compared in clinical studies for UC, PsA, or AS. However, separate studies have found both Xeljanz and Humira to be effective for treating these conditions.

Xeljanz and Humira were compared in a clinical study that looked at people with RA. The study found that treating RA with Xeljanz and methotrexate wasn’t less effective than treating RA with Humira and methotrexate. After 6 months, 46% of people who took Xeljanz and methotrexate had a 50% reduction in their RA symptoms. Of people who took Humira and methotrexate, 44% had the same result.

Costs

Xeljanz and Humira are both brand-name drugs.

Xeljanz may cost less than Humira. The actual price you’ll pay for either drug depends on your insurance plan, your location, and the pharmacy you use.

Like Humira (described above), the drug Enbrel has uses similar to those of Xeljanz. Here’s a comparison of how Xeljanz and Enbrel are alike and different.

Uses

Xeljanz and Enbrel are both approved for use in adults with:

They’re also both used for juvenile idiopathic arthritis in children and adults ages 2 years and older.

Xeljanz is also approved to treat ulcerative colitis (UC) in adults.

Enbrel is also approved to treat plaque psoriasis in people ages 4 years and older.

Drug forms and administration

Xeljanz contains the drug tofacitinib. It comes as a tablet that’s taken by mouth, once or twice a day. It also comes as an oral solution that’s taken twice daily.

Enbrel contains the drug etanercept. It’s given as a subcutaneous injection, typically once every week. You may receive the injection from your healthcare professional, or they may show you how to self-inject the drug at home.

Side effects and risks

Xeljanz and Enbrel contain different drugs. Therefore, they can cause some similar side effects and some different side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Xeljanz, with Enbrel, or with both drugs (when taken individually).

  • Can occur with Xeljanz:
  • Can occur with Enbrel:
    • injection site reactions
  • Can occur with both Xeljanz and Enbrel:
    • diarrhea
    • rash
    • upper respiratory infections, such as the common cold

Serious side effects

These lists contain examples of serious side effects that can occur with Xeljanz, with Enbrel, or with both drugs (when taken individually).

* Xeljanz and Enbrel both have boxed warnings from the FDA regarding the risk of serious infections and cancer. Xeljanz also has a boxed warning regarding the risk of blood clots and increased risk of death. A boxed warning is the strongest warning the FDA requires. It alerts doctors and patients about drug effects that may be dangerous.

Effectiveness

Xeljanz and Enbrel have different FDA-approved uses. However, they’re both used to treat rheumatoid arthritis (RA), psoriatic arthritis (PsA), and ankylosing spondylitis.

These drugs haven’t been directly compared in clinical studies. Separate studies have found both Xeljanz and Enbrel to be effective for treating these conditions.

Costs

Xeljanz and Enbrel are both brand-name drugs.

Xeljanz may cost less than Enbrel. The actual price you’ll pay for either drug will depend on your insurance plan, your location, and the pharmacy you use.

Here are answers to some frequently asked questions about Xeljanz.

Can I take Xeljanz with a biologic?

No, you shouldn’t take Xeljanz or Xeljanz XR with a biologic drug. Biologic drugs are made in a lab from living cells. Many biologics are designed to suppress (decrease) the ability of your immune system to fight infections. This is because biologics are generally used to treat autoimmune disorders, which are caused by your immune system mistakenly attacking your own body.

Taking Xeljanz or Xeljanz XR with biologics can suppress your immune system too much. This can increase your risk of very serious infections that your body won’t be able to fight off.

Talk with your doctor to learn more about which medications are safe to use with Xeljanz or Xeljanz XR.

Will I have withdrawal symptoms if I stop using Xeljanz?

Possibly. If you stop taking either drug, the symptoms that you were using it to treat may come back or become worse.

A small clinical study that included people with rheumatoid arthritis (RA) found that 37% of people who stopped taking Xeljanz were able to stay off the drug for 1 year without their disease getting worse. In this study, people who had less severe RA symptoms were more likely to be able to stop taking Xeljanz without their symptoms worsening.

If you’re interested in stopping Xeljanz or Xeljanz XR treatment, talk with your doctor before doing so. They can discuss with you the risks of stopping treatment.

Does Xeljanz cause mouth sores?

It’s possible that Xeljanz or Xeljanz XR may cause mouth sores.

Xeljanz and Xeljanz XR decrease the ability of your immune system to fight infections. This means that while you’re taking the drug, you have an increased risk for viruses that are already in your body to become reactivated (flare-up). For example, herpes simplex virus (a common virus that causes cold sores) can become active and cause symptoms.

If you have bothersome cold sores while you’re taking Xeljanz or Xeljanz XR, talk with your doctor. They can recommend ways to reduce how often your cold sores occur and how long they last.

How can I prevent infections while I’m taking Xeljanz?

It’s important to try to prevent infections while you’re taking Xeljanz or Xeljanz XR. This is because both are immunosuppressants (drugs that lower your immune system’s ability to fight infections).

The Centers for Disease Control and Prevention (CDC) recommends several easy ways to reduce your risk of getting an infection:

  • Wash your hands with soap and water:
    • before preparing or eating food
    • after changing diapers or using the restroom
    • after touching any items that have been in contact with people who are sick
  • Properly wash and cook your food.
  • Make sure your water is safe to drink.
  • Avoid touching farm animals and the stool of any pets.
  • Avoid swallowing water from any natural bodies of water, such as lakes or rivers.
  • Practice safe sex by using condoms or other barrier methods.

Talk with your doctor about specific ways that you can prevent infections in your daily life.

Should I avoid certain vaccines during Xeljanz treatment?

Yes, you should avoid getting live vaccines during Xeljanz or Xeljanz XR treatment. Live vaccines contain weakened particles of live viruses or bacteria. These particles cause your immune system to react against that particular virus or bacteria. This is how your body develops immunity to protect you from the condition you were vaccinated for.

When you’re taking Xeljanz or Xeljanz XR, your immune system isn’t as effective at fighting infections. If you get a live vaccine during your treatment, you may end up getting infected by the virus or bacteria that the vaccine is meant to protect you from.

Examples of live vaccines include:

Before starting Xeljanz or Xeljanz XR treatment, talk with your doctor about your vaccination history. They’ll make sure that you’re up to date on your vaccines before you start taking either drug.

Xeljanz use before and during pregnancy hasn’t been studied in humans. Some results from animal studies are described below.

Xeljanz use in pregnancy

There isn’t enough information available to know if tofacitinib (the active drug in Xeljanz and Xeljanz XR) is safe to take during pregnancy. In animal studies, harm was seen in fetuses when pregnant animals were given the drug. However, animal studies don’t always predict what will happen in humans.

Keep in mind that there are known risks to fetuses of pregnant people who have active rheumatoid arthritis (RA) or ulcerative colitis (UC). And Xeljanz and Xeljanz XR are used for these conditions.

If you’re pregnant or considering becoming pregnant, talk with your doctor about whether Xeljanz or Xeljanz XR is right for you. Your doctor will discuss the benefits and risks of using either drug during pregnancy. They’ll also discuss the benefits and risks of not treating your condition during pregnancy.

If you’re taking or have taken Xeljanz or Xeljanz XR during pregnancy, you’re encouraged to enroll in the drugs’ pregnancy registry. A pregnancy registry allows healthcare professionals to collect information about the safety of using certain drugs during pregnancy. To enroll in this pregnancy registry, call 877-311-8972 or visit the registry website.

The effect of Xeljanz on fertility

Animal studies have found that tofacitinib (the active drug in Xeljanz and Xeljanz XR) affects the ability of certain animals to become pregnant. It’s not known if this effect is also seen in humans. If you can become pregnant, talk with your doctor before starting the treatment.

It’s not known if Xeljanz or Xeljanz XR is safe to take during pregnancy. If you or your sexual partner can become pregnant, talk with your doctor about your birth control needs while you’re using Xeljanz or Xeljanz XR.

You shouldn’t breastfeed while you’re taking Xeljanz. In animal studies, tofacitinib (the active drug in Xeljanz and Xeljanz XR) did pass into breast milk. It’s not known for sure if this will also happen in humans.

However, it’s recommended that you don’t breastfeed while taking Xeljanz or for at least 18 hours after your last dose of Xeljanz. If you’re taking Xeljanz XR, you shouldn’t breastfeed for at least 36 hours after your last dose of the drug. This is because either drug could possibly cause serious side effects if it’s passed to your child.

If you’re breastfeeding and considering taking Xeljanz or Xeljanz XR, talk with your doctor about other healthy ways to feed your child.

As with all medications, the cost of Xeljanz and Xeljanz XR can vary. The actual price you’ll pay depends on your insurance plan, your location, and the pharmacy you use.

Your insurance company may require you to get prior authorization before they approve coverage for either drug. This means that your doctor will need to send a request to your insurance company asking them to cover the drug. The insurance company will review the request and let you and your doctor know if your plan will cover Xeljanz or Xeljanz XR.

If you’re not sure whether you’ll need to get prior authorization for Xeljanz either treatment, contact your insurance plan.

Financial and insurance assistance

If you need financial support to pay for Xeljanz or Xeljanz XR, or if you need help understanding your insurance coverage, help is available.

Pfizer Inc., the manufacturer of Xeljanz, offers a program called XelSource. For more information and to find out if you’re eligible for support, call 844-935-5269 and say “representative.” To find out more information online, visit the websites below, which are specific for your condition:

You should take Xeljanz or Xeljanz XR according to your doctor or another healthcare professional’s instructions.

The drug is available in these forms:

  • Xeljanz (immediate release), which is released at once in your body after it’s taken. It comes as:
    • oral tablets
    • oral solution
  • Xeljanz XR (extended release), which is released slowly over time in your body after it’s taken. It comes as oral tablets.

When to take Xeljanz

Xeljanz is taken either once a day or twice a day, depending on the form of the drug your doctor prescribes. It can be taken as follows:

  • If you’re taking Xeljanz once a day, it can be taken at any time of the day. But you should take it at the same time each day.
  • If you’re taking Xeljanz twice a day, your two doses should be taken about 12 hours apart. For example, you could take one dose in the morning and one dose in the evening.

Xeljanz XR is only taken once a day. It can be taken at any time of the day. However, you should take it at the same time each day.

To help make sure that you don’t miss a dose, try setting a reminder on your phone. A medication timer may be useful, too.

Taking Xeljanz with food

Xeljanz and Xeljanz XR can each be taken with or without food.

Can Xeljanz be crushed, split, or chewed?

You may be able to crush, split, or chew Xeljanz (immediate-release) tablets. If you have trouble swallowing the tablets, talk with your doctor or pharmacist. They can recommend ways to make swallowing the medication easier for you.

However, you shouldn’t crush, split, or chew Xeljanz XR (extended-release) tablets. These should be swallowed whole. If you have trouble swallowing Xeljanz XR tablets, talk with your healthcare professional. They can recommend ways to help you swallow the tablets, or they may prescribe a different form of Xeljanz for you.

Xeljanz and Xeljanz XR are used to decrease pain and inflammation in people with certain autoimmune disorders.

They’re used in certain adults with:

Xeljanz is also used for certain children ages 2 years and older who have polyarticular juvenile idiopathic arthritis (JIA).

To learn how Xeljanz works to treat these conditions, see this article.

This drug comes with several precautions.

FDA warnings

This drug has boxed warnings. A boxed warning is the most serious warning from the Food and Drug Administration (FDA). It alerts doctors and patients about drug effects that may be dangerous.

  • Risk of serious infections. Xeljanz and Xeljanz XR decrease your immune system’s ability to fight off infections. This may increase your risk of serious infections, such as tuberculosis (TB) or herpes zoster (shingles). Your doctor will check to make sure that you don’t have TB before you start taking Xeljanz or Xeljanz XR. If you have TB or another infection before starting either drug, your doctor may recommend that you wait to start Xeljanz or Xeljanz XR until your infection has been treated.
  • Risk of blood clots and death. People ages 50 years and older with both rheumatoid arthritis (RA) and at least one cardiovascular risk factor have an increased risk of blood clots and death while taking Xeljanz or Xeljanz XR. This risk is increased in people with these conditions who are taking 10 mg of Xeljanz twice a day, compared to people taking lower doses of Xeljanz or using certain other drugs. People with these risk factors shouldn’t take Xeljanz or Xeljanz XR. If you have symptoms of a blood clot while you’re taking either drug, your doctor will advise that you stop taking the medication.
  • Risk of cancer and immune system disorders. Cancer and lymphoma (a type of blood cancer) have occurred in people taking Xeljanz or Xeljanz XR. The risk of immune system disorders is also increased in people who have had a kidney transplant and also are taking either medication with other drugs that decrease their immune system’s ability.
  • Risk of death. Certain people taking Xeljanz or Xeljanz XR may have an increased risk of death, including death caused by a cardiovascular problem. People with RA who are ages 50 years or older and have at least one cardiovascular risk factor may be affected. Your doctor can assess whether this drug is right for you based on your risk factors. They’ll recommend the dosage and length of Xeljanz or Xeljanz XR treatment that’s safest for you.

Other precautions

Before taking Xeljanz or Xeljanz XR, talk with your doctor about your health history. Xeljanz or Xeljanz XR may not be right for you if you have certain medical conditions or other factors affecting your health. These include:

  • Digestive tract problems. Xeljanz or Xeljanz XR may increase your risk of digestive tract perforations (holes in the lining of your stomach or intestines). If you have a history of certain gastrointestinal problems, such as diverticulitis, or you’re using nonsteroidal anti-inflammatory drugs on a regular basis, Xeljanz or Xeljanz XR may not be safe for you. Xeljanz XR may also worsen certain digestive tract problems, such as narrowing or blockages in your intestines. Talk with your doctor to find out if either drug is right for you.
  • Blood disorders. Xeljanz or Xeljanz XR decreases levels of certain blood cells in your body, including red blood cells and two types of white blood cells (called neutrophils and lymphocytes). This can increase your risk of serious infections or anemia. You shouldn’t start taking Xeljanz or Xeljanz XR if you have low levels of these blood cells. Your doctor will check your blood counts before you start either treatment. This allows them to determine whether the drug is safe for you.
  • Severe allergic reaction. Xeljanz and Xeljanz XR have caused severe allergic reactions in some people. These drugs may not be safe for you if you’ve had a severe allergic reaction to either in the past. If you’re unsure whether you’ve had a severe allergic reaction to Xeljanz or Xeljanz XR, talk with your doctor.
  • Liver problems. Xeljanz and Xeljanz XR may not be safe for people with severe liver disease or liver damage, including hepatitis B and hepatitis C. If you have liver problems, talk with your doctor about whether Xeljanz or Xeljanz XR is right for you.
  • Kidney problems. The level of these drugs in your bloodstream may be increased in people with moderate or severe kidney damage. If you have any problems with your kidneys, talk with your doctor before starting Xeljanz or Xeljanz XR treatment. They may adjust your dosage of this drug if you have kidney damage.
  • Pregnancy. It’s not known how safe Xeljanz or Xeljanz XR is to take during pregnancy. For more information, please see the “Xeljanz and pregnancy” section above.
  • Breastfeeding. You shouldn’t breastfeed while you take Xeljanz or Xeljanz XR. For more information, please see the “Xeljanz and breastfeeding” section above.

Note: For more information about the potential negative effects of Xeljanz and Xeljanz XR, see the “Xeljanz side effects” section above.

Using more than the recommended dosage of Xeljanz or Xeljanz XR can lead to serious side effects.

What to do in case of overdose

If you think you’ve taken too much of this drug, call your doctor. You can also call America’s Poison Centers at 800-222-1222 or use its online tool. But if your symptoms are severe, call 911 or go to the nearest emergency room right away.

When you get Xeljanz or Xeljanz XR from the pharmacy, the pharmacist will add an expiration date to the label on the medication. This date is typically 1 year from the date they dispensed it.

The expiration date helps guarantee the effectiveness of the medication during this time. The current stance of the Food and Drug Administration (FDA) is to avoid using expired medications. If you have unused medication that has gone past the expiration date, ask your pharmacist how to correctly dispose of it.

Note that Xeljanz oral solution expires 60 days after you open the bottle.

Storage

How long a medication remains good can depend on many factors, including how and where you store the medication.

Xeljanz and Xeljanz XR should be stored at room temperature (68°F to 77°F/20°C to 25°C) in a tightly sealed container away from light. Avoid storing this medication in areas where it could get damp or wet, such as in bathrooms.

Disposal

If you no longer need to take Xeljanz and have leftover medication, it’s important to dispose of it safely. This helps prevent others, including children and pets, from taking the drug by accident. It also helps keep the drug from harming the environment.

The FDA website provides several useful tips on medication disposal. You can also ask your pharmacist for information on how to dispose of your medication.

The following information is provided for clinicians and other healthcare professionals.

Indications

Xeljanz and Xeljanz XR are approved by the Food and Drug Administration (FDA) for use in adults with any of the following:

  • moderately to severely active ulcerative colitis (UC), if tumor necrosis factor (TNF) blockers were ineffective or intolerable for them
  • moderately to severely active rheumatoid arthritis (RA), if TNF blockers were ineffective or intolerable for them
  • active psoriatic arthritis (PsA), if TNF blockers were ineffective or intolerable for them
  • active ankylosing spondylitis (AS), if TNF blockers were ineffective or intolerable for them

In addition, Xeljanz is approved for use in children ages 2 years and older who have active polyarticular juvenile idiopathic arthritis and in whom TNF blockers were ineffective or intolerable.

Xeljanz and Xeljanz XR have certain limitations of use with regard to combination therapy. For details, see the prescribing information.

Mechanism of action

Xeljanz and Xeljanz XR contain the drug tofacitinib, which is a Janus kinase (JAK) inhibitor. JAK is an intracellular enzyme that activates Signal Transducers and Activators of Transcription (STATs), which are modulators of gene expression that stimulate hematopoiesis and immune cell function. Xeljanz and Xeljanz XR inhibit the JAK enzyme, thereby repressing STAT activity and immune cell activation.

Pharmacokinetics and metabolism

Following oral administration, the bioavailability of Xeljanz is 74%. Peak plasma concentrations are reached within 0.5 to 1 hour for Xeljanz and within 4 hours for Xeljanz XR. Steady-state concentrations are achieved after approximately 24 to 48 hours for Xeljanz and 48 hours for Xeljanz XR.

Protein binding is about 40%, primarily to albumin. The majority of Xeljanz metabolism occurs via CYP3A4, with minority occurring via CYP2C19. Elimination half-life is about 3 hours for Xeljanz and about 6 hours for Xeljanz XR.

Contraindications

There are no contraindications to Xeljanz or Xeljanz XR use.

Storage

Xeljanz and Xeljanz XR should be stored in the original container at room temperature (68°F to 77°F/20°C to 25°C).

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or another healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.