FDA Approves High-Dose, Extended-Release Version of Xeljanz, Despite Blood Clot Risks

Although concerns emerged earlier this year about the risk of severe and potentially life-threatening blood clots from Xeljanz side effects when used at a 10 mg dose, federal regulators have approved new extended-release versions of the drug, which delivers even higher doses, for use among individuals with ulcerative colitis.

Pfizer Inc. issued a press release on this month, announcing the FDA’s approval of Xeljanz XR extended-release tablets in 11 mg and 22 mg doses, specifically for treatment of patients with moderate to severely active ulcerative colitis.

The new doses are meant to specifically be used by ulcerative colitis patients who have had an inadequate response or have an intolerance to a class of drugs known as TNF blockers which are typically prescribed to treat the condition.

Xeljanz (tofacitinib) was first approved by the FDA in 2012, to treat adults with rheumatoid arthritis, an autoimmune disorder that causes inflammation of the joints in approximately one percent of the population. The drug was designed to block the activity of certain enzymes in the body that affect immune system function and is commonly used as an alternative for patients who have tried methotrexate and other medications without success.

Use of the medication was expanded in December 2017, after the FDA authorized use of Xeljanz and Xeljanz XR for the treatment of active psoriatic arthritis (PsA), and then approval was expanded again in May 2018 to include treatment of moderate to severe active ulcerative colitis. Generally, it is given at the 5 mg per day dose to treat arthritis, and at 10 mg per day to treat ulcerative colitis.

The FDA now recommends the 10 mg dose not be used in patients with ulcerative colitis, unless there is no suitable alternative.

The new extended release tablets are meant to be given once per day, for eight weeks, or up to a maximum of 16 weeks as induction therapy. Pfizer indicates the lowest effective dose should be used, and that the higher doses of the medication should be limited to the shortest possible duration, with “careful consideration of benefits and risks to the individual patient.”

Xeljanz Blood Clot Lawsuits

The new version and warnings come as Pfizzer faces a number of Xeljanz lawsuits filed by individuals who claim the drug maker previously withheld warnings about the blood clot risk, indicating that they may have avoided a pulmonary embolism, deep vein thrombosis or other injuries if earlier information had been provided to users and the medical community.

In February 2019, preliminary data from a Xeljanz clinical trial was released, indicating that patients receiving 10mg doses of Xeljanz twice per day were found to have a significantly higher risk of experiencing pulmonary embolisms and had an overall higher rate of mortality when compared to patients taking 5mg doses of Xeljanz for ulcerative colitis.

In response, the FDA issued a warning about the Xeljanz blood clot problems. A few months later, the agency announced a black box label warning for Xeljanz, in July 2019.

Since Xeljanz was first introduced into the market in 2012 by Pfizer Pharmaceutical Company, roughly 1% of the population is anticipated to have used or currently be using the medication. The company’s multi-purpose drug has been steadily increasing in sales each year, reaching blockbuster status with sales in excess of $1 billion per year.