In medicine, a biologic refers to a substance made from a living organism or its products. They are used to prevent, diagnose, or treat a disease. Biological drugs include antibodies, interleukins, and vaccines. Xeljanz is an oral medication used to treat certain inflammatory conditions such as rheumatoid arthritis and ulcerative colitis. While it may have some of the same adverse events as biologics, it is not considered a true biologic.
So how does Xeljanz work, what are some side effects, and what makes it different from biologics?
What medical conditions does Xeljanz treat?
Xeljanz (tofacitinib) is a brand-name medication manufactured by Pfizer, Inc. It is approved by the U.S. Food and Drug Administration (FDA) to treat adults with:
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Moderate to severe active rheumatoid arthritis (RA)
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Active psoriatic arthritis (PsA), a type of arthritis approximately 30% of people with psoriasis develop
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Active ankylosing spondylitis, a type of inflammatory disease that can cause chronic pain and stiffness in the spine and hips
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Moderate to severe active ulcerative colitis (UC)
It is also FDA-approved to treat:
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Polyarticular course juvenile idiopathic arthritis (pcJIA) in pediatric patients 2 years of age and older
Xeljanz is typically given to patients who have had an inadequate response or failed one or more tumor necrosis factor or TNF blockers such as Humira (adalimumab). It can be used alone or with other arthritis medications such as Rheumatrex (methotrexate). However, the use of Xeljanz along with biologic disease-modifying antirheumatic drugs (DMARDs) or potent immunosuppressants such as Imuran (azathioprine) and Neoral (cyclosporine) should be avoided as it can increase your risk of serious infections.
How does Xeljanz work?
Xeljanz’s active ingredient, tofacitinib, is known as a Janus kinase, or JAK inhibitor. JAKs are enzymes found inside many cells in your body, including your bones and joints. They transmit signals that play a role in activating your body's immune system. By blocking JAKs, Xeljanz stops the inflammatory process. This helps relieve symptoms such as pain and swelling associated with rheumatoid arthritis and other inflammatory conditions.
What doses of Xeljanz are available?
Xeljanz is available in several dosage forms and strengths, including:
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Xeljanz 5 mg and 10 mg tablets
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Xeljanz XR 11 mg and 22 mg extended-release tablets
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Xeljanz 1 mg/mL oral solution
How do you use Xeljanz?
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Read the Medication Guide and Prescribing Information that comes with this medication.
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Xeljanz tablets and Xeljanz oral solution is taken twice a day with or without food.
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Xeljanz XR tablets are taken once a day with or without food.
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Xeljanz XR tablets should be swallowed whole. Do not split, crush, or chew Xeljanz XR tablets.
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After taking Xeljanz XR, you may see something in your stool that looks like a tablet. There is no need for alarm as it is the empty shell of the Xeljanz XR tablet left after the medication has been absorbed by your body.
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If you think you have taken too much Xeljanz, call your healthcare provider or go to the nearest emergency room immediately.
What drug interactions are there with Xeljanz?
When Xeljanz is taken with other medications, it can change how they work or make some side effects more likely or severe. You should ask your healthcare provider if any of the prescription medications, over-the-counter (OTC) drugs, vitamins, or supplements you take may interact with Xeljanz, including:
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CYP3A4 inhibitors such as ketoconazole and fluconazole
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CYP3A4 inducers such as rifampin
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Immunosuppressant medications such as azathioprine, cyclosporine, and tacrolimus
What are the side effects of Xeljanz?
The most common side effects of Xeljanz when compared to placebo during clinical trials were:
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Upper respiratory tract infection
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Diarrhea
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Nausea
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Common cold symptoms
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Headache
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High cholesterol levels
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Herpes zoster infection (shingles)
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High blood pressure
Sometimes, Xeljanz can cause more serious side effects, including:
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Serious, life-threatening allergic reactions
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Increased risk of death from cardiovascular problems such as heart attack, stroke, and blood clots (thrombosis)
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Increased risk of certain cancers including lymphoma, lung cancer, breast cancer, skin cancer, and other malignancies
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Stomach problems including perforations (holes) in your stomach or intestines, especially in those taking NSAIDs (nonsteroidal anti-inflammatory drugs), corticosteroids, or methotrexate
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Low red blood cells (anemia)
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Liver damage and increased liver enzymes
Contact your healthcare professional for medical advice about any possible adverse effects you experience while taking Xeljanz. You can report your adverse effects to the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Are there any Boxed Warnings with Xeljanz?
The FDA has approved the following Boxed Warning labeling for Xeljanz:
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Xeljanz can lower your immune system’s ability to fight infections. Some people have developed serious infections including tuberculosis (TB), and other infections that can spread throughout the body and possibly cause death. You should be tested for TB before starting Xeljanz and closely monitored for symptoms of TB while taking Xeljanz.
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There is an increased risk of death from serious cardiovascular (heart) events in people 50 years of age and older who have at least 1 heart-related risk factor and are taking Xeljanz twice a day.
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Lymphoma and other cancers including skin cancers have occurred in people taking Xeljanz. Be sure to let your doctor know if you have a personal or family history of cancer.
Are there any other precautions with Xeljanz?
Before beginning Xeljanz, make sure your healthcare provider is aware of your medical conditions, including:
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Active infection
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Are a current or previous smoker
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Personal or family history of cancer
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Previous heart attack, stroke, or blood clot
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Liver problems including hepatitis B
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Kidney problems
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Diverticulitis or ulcers in your stomach or intestines
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A known allergy to tofacitinib or any ingredients in the Xeljanz formulation
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Recently received or are scheduled to receive a live vaccine
How quickly does Xeljanz start working?
In clinical studies, Xeljanz reduced symptoms of rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and juvenile idiopathic arthritis in as little as two weeks for some people. For other people, it may take 3 to 6 months to work.
For people with ulcerative colitis, Xeljanz started working within three days, with significant improvement in symptoms within two weeks of beginning treatment.
What is the difference between Humira and Xeljanz?
Xeljanz is an oral medication that works differently from the injectable medication Humira (adalimumab) to reduce joint pain and swelling caused by rheumatoid arthritis.
Xeljanz is a JAK inhibitor that works by blocking the actions of JAK proteins, which can cause inflammation in the joints and other parts of the body. Humira is a tumor necrosis factor (TNF) inhibitor or a biologic. TNF is a protein that causes inflammation and is found in high levels in the joints of people with rheumatoid arthritis. By blocking TNF, Humira reduces inflammation and joint pain.
While there aren’t many studies comparing the 2 medications, one study showed that people taking Xeljanz with methotrexate had just as much symptom relief as those taking Humira and methotrexate.
Xeljanz and Humira have many of the same side effects such as an increased risk of serious infections. However, Xeljanz may increase your risk of major heart problems and certain types of cancer more than Humira.
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