FDA Clears Extended-Release Tofacitinib (Xeljanz XR) for RA

The US Food and Drug Administration (FDA) has approved tofacitinib citrate extended-release (Xeljanz XR, Pfizer Inc) 11-mg tablets for once-daily treatment of moderate to severe rheumatoid arthritis (RA) in patients who have not responded adequately to, or are intolerant of, methotrexate, Pfizer has announced.

In 2012, tofacitinib (Xeljanz) became the first selective oral Janus kinase (JAK) inhibitor to be approved by the FDA. The drug interrupts signaling of several cytokines involved in immune response.

Xeljanz XR provides patients with RA a new once-daily oral dosing option. It is the first and only once-daily oral JAK inhibitor available for patients with moderate to severe RA, Pfizer said in a news release.

"Xeljanz XR 11 mg administered once daily is pharmacokinetically equivalent to Xeljanz 5 mg administered twice daily," Kelly Sinclair, media relations, GCI Health, on behalf of Pfizer, noted in an email to Medscape Medical News.

"The availability of Xeljanz XR provides physicians with a new treatment option for people with RA who may prefer an oral once-daily treatment," Roy Fleischmann, MD, clinical professor, Department of Internal Medicine, University of Texas Southwestern Medical Center and co-medical director, Metroplex Clinical Research Center, Dallas, said in the release.

The efficacy and safety profile of tofacitinib has been studied in roughly 6200 patients with moderate to severe RA, amounting to more than 19,400 patient-years of drug exposure in the global clinical development program, Pfizer said.

The most common adverse reactions in clinical trials were upper respiratory tract infections, headache, diarrhea, and inflammation of the nasal passage and the upper part of the pharynx.

In clinical trials, tofacitinib was associated with an increased risk for serious infections, including opportunistic infections, tuberculosis, cancers, and lymphoma. The drug carries a boxed warning regarding these safety risks. The drug is also associated with increases in cholesterol and liver enzyme test results and decreases in blood counts. The FDA approved tofacitinib with a risk evaluation and mitigation strategy.


The term arthritis refers to stiffness in the joints. See Answer

FDA Clears Extended-Release Tofacitinib (Xeljanz XR) for RA. Medscape. Feb 24, 2016.

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