Xeljanz (Tofacitinib) – Oral

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.

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.

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.

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?

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.

Precautions

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:

• Drugs that decrease the activity of CYP3A4, which include antibiotics Biaxin XL (clarithromycin) and ketoconazole
• Drugs that increase the activity of CYP3A4, which include phenobarbital and Dilantin (phenytoin)

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).

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.