Medically Reviewed by Goldina I. Erowele, MBA, PharmD on June 28, 2024
Written by Ami Ishver, PharmDManaging symptoms of rheumatoid arthritis may require trying different medicines to see what works best for you and your symptoms. The approval of Xeljanz has led to changes in how rheumatoid arthritis is managed.
Xeljanz (ZEL’ JANS’) was approved in 2012 and was the first by-mouth Janus kinase (JAK) inhibitor in its class. Xeljanz is approved to treat adults with mild to moderate rheumatoid arthritis (RA) who have taken a medicine called a t umor necrosis factor (TNF) inhibitor and either could not tolerate the medicine or the medicine did not work for their rheumatoid arthritis.
TNF inhibitors are medicines that are either injected at home or can be given to you by your doctor through an IV infusion. Medicines such as Xeljanz have allowed people a by-mouth treatment option for their rheumatoid arthritis.
Rheumatoid arthritis is an autoimmune disease that affects your joints. An autoimmune disease is where your body starts to attack your tissues. In rheumatoid arthritis, specifically, the joints are affected and can cause inflammation, pain, redness, swelling, stiffness, and warmth. There is no cure for rheumatoid arthritis, but medicines can help slow down the progression of the disease and can help manage symptoms.
Rheumatoid arthritis can affect the joints on both sides of your body including your hands, wrists, and knees. Over time, rheumatoid arthritis can affect other parts of your body such as your heart, lungs, and blood vessels.
The active ingredient in Xeljanz is tofacitinib, which is a JAK inhibitor. JAK inhibitors belong to a class of medicine called biologic disease-modifying antirheumatic drugs (DMARDs), which regulate the immune system. Xeljanz regulates your overactive immune system by interrupting the pathway in the cell that is believed to cause inflammation. This can reduce inflammation, which can relieve joint pain, swelling, stiffness, and can help stop further joint damage.
For the treatment of rheumatoid arthritis, the recommended dosing in adult patients is 5 milligrams twice a day if you are taking the tablet, or 11 milligrams per day if you are taking the extended-release tablet. Xeljanz extended-release tablets (Xeljanz XR) work over a longer period of time. Because of this, the dosing of Xeljanz XR is different from Xeljanz. Xeljanz and Xeljanz XR can be taken with or without food.
If you are taking certain medicines that may affect the blood levels of Xeljanz or have kidney or liver problems, your health care provider may modify your dose. If you have certain blood disorders, your health care provider may temporarily pause your Xeljanz dose or stop it completely. Take Xeljanz as prescribed by your health care provider.
If you are taking Xeljanz XR, you may see something in your stool called a residual tablet shell. A residual tablet shell is the shell of a tablet that you see after the medicine has been absorbed by the body.
Six clinical studies looked at the safety and efficacy of Xeljanz in people with moderate to severe rheumatoid arthritis. The average age of people in these studies was between 48 and 56. Over three-quarters of the people in the study were female.
The first clinical study was a 6-month study in people who were not seeing benefits from (biologic or nonbiologic) DMARDs. People received Xeljanz 5 milligrams or 10 milligrams twice daily and were compared to people who took a placebo containing no medicine.
Three tests were done in the study. The study looked to see the number of people who achieved a 20% improvement in the American College of Rheumatology scale (ACR20) from baseline to 3 months, meaning the number of people who had at least a 20% improvement in their rheumatoid arthritis symptoms.
The study also looked at the change from baseline to 3 months in Health Assessment Questionnaire–Disability Index (HAQ-DI) scores, which looks at the ability to accomplish certain daily activities, with a higher score indicating greater disability.
The study also looked at the rate of people with Disease Activity Score for 28-joint counts based on the erythrocyte sedimentation rate (DAS28-4[ESR]) of less than 2.6 from baseline to 3 months. A score of 2.6 or less meant that a person’s symptoms were under control ( remission ).
The second clinical study was done over 2 years and looked at people who have never taken methotrexate. People in the study were either taking Xeljanz 5 milligrams or 10 milligrams twice daily or methotrexate up to 20 milligrams per week. The study looked at ACR70 from baseline to month 6, meaning the number of people who had at least a 70% improvement in their rheumatoid arthritis symptoms. The study also looked at the change in van der Heijde-modified total Sharp Score (mTSS) from baseline to month 6. The mTSS score measures the degree of joint damage, with a higher score indicating more joint damage.
Xeljanz plus other medicines for rheumatoid arthritis
The third clinical study was a 12 month study conducted in people who were not seeing benefits from (biologic or nonbiologic) DMARDs. People in the study were taking a non-biologic DMARD (primarily methotrexate ) and were taking either Xeljanz 5 milligrams or 10 milligrams twice daily, or placebo. Methotrexate is a medicine that can be used to treat rheumatoid arthritis. The number of people who achieved an ACR20 response and rate of DAS28-4(ESR) less than 2.6 were looked at from baseline to month 6, and HAQ-DI was looked at from baseline to month 3.
The fourth clinical study was done over 12 months and looked at people who were not seeing benefits from methotrexate. Everyone in the study was taking methotrexate and were either taking Xeljanz 5 milligrams or 10 milligrams twice daily, adalimumab 40 milligrams (another medicine used to treat rheumatoid arthritis) every other week, or placebo. The number of people who achieved an ACR20 response and rate of DAS28-4(ESR) less than 2.6 were looked at from baseline to month 6, and HAQ-DI was looked at from baseline to month 3.
The fifth clinical study was done over 2 years and looked at people who were not seeing benefits from methotrexate. Everyone in the study was taking methotrexate and were either taking Xeljanz 5 milligrams or 10 milligrams twice daily or placebo. The number of people who achieved an ACR20 response and rate of DAS28-4(ESR) less than 2.6 and change in mTSS were looked at from baseline to month 6, and HAQ-DI was looked at from baseline to month 3.
The sixth clinical study was done over 6 months and looked at people who were not seeing benefits from a TNF inhibitor . Everyone in the study was taking methotrexate and were either taking Xeljanz 5 milligrams or 10 milligrams twice daily or placebo. The number of people who achieved an ACR20 response rate of DAS28-4(ESR) less than 2.6 and HAQ-DI were looked at from baseline to month 3.
Xeljanz 5 milligrams twice daily is the recommended dose for rheumatoid arthritis. Xeljanz 10 milligrams twice daily is not the recommended dose for the treatment of rheumatoid arthritis.
Improvement in rheumatoid arthritis symptoms. People who took Xeljanz had an improvement in their rheumatoid arthritis symptoms, meaning they had reduced joint pain and swelling.
Joint damage. In people with moderate to severe rheumatoid arthritis, Xeljanz slowed down the progression of joint damage.
Physical function. Xeljanz improved people’s physical function, meaning people were able to accomplish certain daily activities (such as dressing and grooming, eating, walking, hygiene, reaching and gripping) more easily.
The effects of Xeljanz and Xeljanz XR may be seen a few weeks to a few months after taking the medicine. You should start to notice less swelling, pain, and stiffness in your joints. Talk to your health care provider if you are still experiencing symptoms that are bothering you. Your health care provider may add other medicines or change your medicines to manage your rheumatoid arthritis.
The most common side effects seen with Xeljanz are an infection in the nose or throat, sore throat, common cold symptoms, diarrhea, and headache.
Infection in the nose or throat, sore throat, or the common cold may happen while taking Xeljanz. Taking over-the-counter medicines may help manage your symptoms. Talk to your health care provider if your symptoms do not improve or get worse.
Diarrhea may occur while you are taking Xeljanz. To limit diarrhea, you can try simple steps such as eating bland foods like rice, bananas, and toast, drinking plenty of water, and lowering the amount of caffeine you are drinking. Call your health care provider if your diarrhea symptoms are not improving or are becoming worse.
If you are experiencing headaches from Xeljanz, taking over-the-counter pain medicines such as acetaminophen or ibuprofen can help. Call your health care provider if your headaches are not getting better or are becoming worse.
Taking Xeljanz with certain medicines called CYP3A4 and CYP2C19 inhibitors can increase the level of Xeljanz in your blood and can increase your risk of side effects. These medicines include fluconazole and ketoconazole, which are used to treat fungal infections. Your health care provider may adjust the dose of Xeljanz if you are taking medicines that affect the level of Xeljanz in your blood.
Taking certain medicines called CYP3A4 inducers (such as rifampin) can lower the level of Xeljanz in your blood and may cause Xeljanz not to work as well. It is not recommended to take these medicines with Xeljanz.
It is not recommended to take Xeljanz with other medicines that suppress your immune system. These medicines may include immunosuppressants such as azathioprine, cyclosporine, or tacrolimus. Taking Xeljanz with immunosuppressants can potentially over-suppress your immune system and may increase your risk of developing infections.
It is also not recommended to take Xeljanz with biologic DMARDs. These can include:
Biologic DMARDs are commonly prescribed in people with different types of inflammatory conditions such as arthritis or ulcerative colitis (UC). Taking Xeljanz with biologic DMARDs can potentially over-suppress your immune system and may increase your risk of developing infections. Talk to your health care provider about your health conditions and all the medicines that you are taking.
