Arthritis Treatment What to Know About Xeljanz (Tofacitinib) The First JAK Inhibitor for Rheumatoid Arthritis By Carol Eustice Carol Eustice Facebook Carol Eustice is a writer covering arthritis and chronic illness, who herself has been diagnosed with both rheumatoid arthritis and osteoarthritis. Learn about our editorial process Updated on November 11, 2020 Medically reviewed Verywell Health articles are reviewed by board-certified physicians and healthcare professionals. These medical reviewers confirm the content is thorough and accurate, reflecting the latest evidence-based research. Content is reviewed before publication and upon substantial updates. Learn more. by Grant Hughes, MD Medically reviewed by Grant Hughes, MD LinkedIn Grant Hughes, MD, is board-certified in rheumatology and is the head of rheumatology at Seattle's Harborview Medical Center. Learn about our Medical Expert Board Print Table of Contents View All Table of Contents Uses Before Taking Dosage Side Effects Warnings and Interactions Xeljanz (tofacitinib citrate) is an oral Janus kinase (JAK) inhibitor—a type of disease-modifying anti-rheumatic drug (DMARD)—used to treat moderately to severely active rheumatoid arthritis (RA) in adults. Typically prescribed after unsuccessful treatment with methotrexate, Xeljanz relieves joint pain, inflammation, and stiffness by reducing immune system activity through a different therapeutic pathway than other DMARDs. Xeljanz is available in both immediate- and extended-release formulations. There is no generic. Uses Xeljanz is approved to treat rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. It can be used alone (as monotherapy) or combined with methotrexate or other non-biologic DMARDs. Approved by the Food and Drug Administration (FDA) in 2012, Xeljanz is considered a small-molecule medication, not a biologic drug. Biologics block pro-inflammatory cytokines from outside the cell while Xeljanz works from the inside. Xeljanz inhibits the JAK pathway—a signaling pathway inside cells that plays a significant role in inflammation associated with rheumatoid arthritis. JAKs are intracellular enzymes that transmit signals that arise from cytokine or growth factor-receptor interactions on the cell membrane. In clinical trials, Xeljanz alone or in combination with another DMARD was shown to significantly reduce the signs and symptoms of RA and improve the ability to perform typical daily activities. Potent Corticosteroid Drugs Tame Inflammation Quickly Before Taking Xeljanz is indicated in rheumatoid arthritis treatment after methotrexate has failed to bring the disease into remission. Prior to prescribing Xeljanz, your healthcare provider will go over your medical history, including your current RA symptoms and previous treatment regimens. In addition, your healthcare provider will perform skin tests to check for tuberculosis and run blood tests to check your cholesterol levels, liver enzymes, and blood cell counts. Baseline levels will be recorded before you start therapy with Xeljanz so they can be referenced later. Periodic laboratory tests are recommended throughout the duration of treatment because Xeljanz may cause changes to certain types of white blood cells, hemoglobin, liver enzymes, and lipids. You may also need to update your vaccinations prior to treatment with Xeljanz, as live-virus vaccines must be avoided while taking the drug. These vaccines include: Shingles FluMist influenza nasal spray Measles, mumps, and rubella Yellow fever What to Ask a Healthcare Provider Before Taking a New Medication Precautions and Contraindications Your healthcare provider will go over the potential benefits and risks of this drug with you prior to prescribing the treatment. Xeljanz may pose more of a risk to people with certain conditions. Tell your healthcare provider if you are age 50 or older, a smoker or former smoker, or have or have ever had: Cancer Diabetes Heart attack or other heart problems Stroke or blood clots High cholesterol High blood pressure HIV or AIDS Infections that are frequent, chronic, or come and go, whether systemic or local, such as open wounds, sores, and cold sores Liver disease Kidney transplant Lung disease Other immune system disorders Tuberculosis Gastrointestinal perforations In addition, let your healthcare provider know if you live or have ever lived in areas where the fungal infection histoplasmosis is more common, such as the Ohio or Mississippi River valleys, parts of Central and South America, Africa, Asia, and Australia. Adequate studies of Xeljanz in pregnant women have not been performed. Xeljanz should only be used during pregnancy if the benefit of the drug outweighs the potential risk to the fetus. Comorbidity May Affect Treatment Decisions for Arthritis Dosage Regular Xeljanz is to be taken twice daily—5 milligrams (mg) per dose. Xeljanz-XR, the extended-release version, comes as an 11-mg tablet that is taken once daily. Xeljanz can be taken with or without food and should be swallowed whole. Do not chew, split, or crush it. If you miss a dose, take it as soon as you remember unless it is almost time for the next dose. In that case, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. Ask your healthcare provider or pharmacist if you have any questions. Side Effects The most common adverse effects associated with Xeljanz, which occurred during the first three months of use in clinical trials, were: Upper respiratory tract infections Headache Diarrhea Stuffy or runny nose Tell your healthcare provider if these symptoms are severe or do not go away. Xeljanz may increase your cholesterol levels. Your healthcare provider will monitor your cholesterol closely while you are taking this medication. Severe There are also some serious side effects associated with taking Xeljanz. If you experience any of the following, call your healthcare provider immediately or seek emergency medical treatment: Hives Swelling of face, eyes, lips, or throat Difficulty swallowing or breathing Stomach pain accompanied by fever and diarrhea or constipation Yellowing of the skin or eyes Loss of appetite Dark urine Clay-colored bowel movements Vomiting Rash Pale skin Shortness of breath Warnings and Interactions Xeljanz carries a black box warning for serious and potentially deadly adverse events. These include: Serious infections leading to hospitalization or death, such as tuberculosis, bacterial, invasive fungi, viral, and other opportunistic infections Serious heart-related events, blood clots, and death Lymphoma and other malignancies Epstein-Barr virus–associated lymphoproliferative disorder Xeljanz should not be taken alongside biologic drugs. These include: Enbrel (etanercept) Remicade (infliximab) Humira (adalimumab) Cimzia (certolizumab pegol) Simponi (golimumab) Orencia (abatacept) Actemra (tocilizumab) Rituxan (rituximab) Kineret (anakinra) Some medications should be used with caution when taking Xeljanz and may require your healthcare provider to alter your dosage or monitor you for side effects including liver damage. These include: Nonsteroidal anti-inflammatory medications (NSAIDs) such as aspirin, Advil or Motrin (ibuprofen), and Naprosyn or Aleve (naproxen) Azasan, Imuran (azathioprine) Gengraf, Neoral, Sandimmune (cyclosporine) Otrexup, Rasuvo, Trexall (methotrexate) Steroids including dexamethasone, Medrol (methylprednisolone), Prelone (prednisolone), and prednisone Diflucan (fluconazole) Onmel, Sporanox (itraconazole) Xolegel (ketoconazole) Carbatrol, Tegretol, Equetro (carbamazepine) Biaxin (clarithromycin) Crixivan (indinavir) Viracept (nelfinavir) Nefazodone Phenobarbital Dilantin/Phenytek (phenytoin) Mycobutin (rifabutin) Rifadin/Rimactane (rifampin) What's Available for Treating Rheumatoid Arthritis? Was this page helpful? Thanks for your feedback! Dealing with chronic inflammation? An anti-inflammatory diet can help. Our free recipe guide shows you the best foods to fight inflammation. Get yours today! Sign Up You're in! Thank you, {{form.email}}, for signing up. There was an error. Please try again. What are your concerns? Other Inaccurate Hard to Understand Submit 6 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. American College of Rheumatology. Tofacitinib Citrate (Xeljanz). U.S. National Library of Medicine: MedlinePlus. Tofacitinib. UpToDate. Tofacitinib: Drug information. Dhillon S. Tofacitinib: A Review in Rheumatoid Arthritis. Drugs. 2017;77(18):1987-2001. doi:10.1007/s40265-017-0835-9 Singh JA, Saag KG, Bridges SL Jr, et al. 2015 American College of Rheumatology Guideline for the Treatment of Rheumatoid Arthritis. Arthritis Rheumatol. 2016;68(1):1-26. doi:10.1002/art.39480 U.S. Centers for Disease Control and Prevention. Histoplasmosis.