Tofacitinib citrate (Xeljanz)

What is Tofacitinib citrate (Xeljanz)? What is Xeljanz used for?

Tofacitinib is an oral drug used for treating rheumatoid arthritis. It belongs to a class of drugs called Janus kinase (JAK) inhibitors. JAKs are enzymes (proteins) that regulate chemical signaling pathways that control biologic processes such as blood formation and the immune response that causes the pain, tenderness and swelling of inflammation.

JAKs are found in many cells, especially stem cells in bones and joints. Inhibition of JAKs by tofacitinib prevents inflammation and tissue destruction that is associated with the inflammation of rheumatoid arthritis. Tofacitinib was approved in November 2012.

What brand names are available for Tofacitinib citrate (Xeljanz)?


Is Tofacitinib citrate (Xeljanz) available as a generic drug?


Do I need a prescription for Tofacitinib citrate (Xeljanz)?


What are the side effects of Tofacitinib citrate (Xeljanz)?

Side effects of tofacitinib are:

Tofacitinib carries a boxed warning of risk of developing infections that may lead to hospitalization or death.

Patients must be carefully monitored for the development of signs and symptoms of infection before and during the treatment of tofacitinib.

What is the dosage for Tofacitinib citrate (Xeljanz)?

The recommended dose in adults is: One tablet (5 mg) by mouth twice daily with or without food.

Safe and effective use of tofacitinib is not established in pediatric patients.


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

Which drugs or supplements interact with Tofacitinib citrate (Xeljanz)?

Ketoconazole (Nizoral, Extina, Xolegel, Kuric) and fluconazole (Diflucan) slow down the metabolism (elimination) of tofacitinib, increasing tofacitinib levels in the body.

Rifampin accelerates tofacitinib metabolism, which can reduce the beneficial effects of tofacitinib.

Combining tofacitinib with other medications like azathioprine (Imuran, Azasan), cyclosporine, tacrolimus (Prograf), or oral steroids may cause further suppression of the immune system.

Is Tofacitinib citrate (Xeljanz) safe to take if I'm pregnant or breastfeeding?

There are no adequate studies of tofacitinib to determine safe and effective use in pregnant women.

It is not known whether tofacitinib enters breast milk; therefore, it is best to be cautious before using it in nursing mothers.

What else should I know about Tofacitinib citrate (Xeljanz)?

What preparations of Tofacitinib citrate (Xeljanz) are available?

Tofacitinib is available as film-coated, immediate-release, 5 mg tablets.

How should I keep Tofacitinib citrate (Xeljanz) stored?

Tofacitinib should be stored at room temperature between 20 C to 25 C (68 F to 77 F).


Tofacitinib citrate (Xeljanz) is an oral medication prescribed to treat rheumatoid arthritis. Side effects, drug interactions, dosage, and pregnancy safety information should be reviewed prior to taking this medication.

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Medically reviewed by John P. Cunha, DO, FACOEP; Board Certified Emergency Medicine


Xeljanz Prescribing Information.