What is the use of Tofacitinib (Xeljanz)?

From the Guidelines

Tofacitinib (brand name Xeljanz) is an oral Janus kinase (JAK) inhibitor used to treat moderate to severe rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis, with a typical dosage of 5 mg twice daily for rheumatoid and psoriatic arthritis, or 10 mg twice daily for ulcerative colitis induction therapy (followed by 5 mg twice daily for maintenance) 1.

Key Points

• Tofacitinib works by blocking JAK enzymes that contribute to inflammation, thereby reducing pain, swelling, and disease progression 1.
• Patients should be screened for tuberculosis and other infections before starting treatment, as the medication increases infection risk 1.
• Other potential side effects include elevated cholesterol levels, gastrointestinal perforations, and increased risk of blood clots and certain cancers 1.
• Tofacitinib should not be combined with other potent immunosuppressants, and live vaccines should be avoided during treatment 1.
• The medication may take 4-8 weeks to show full effectiveness, and patients should not stop taking it abruptly without consulting their healthcare provider 1.

Important Considerations

• The use of tofacitinib in patients with prior failure or intolerance to TNF antagonists is recommended by the FDA 1.
• In Europe, the European Medicines Agency recommends cautious use of JAK inhibitors as a first-line agent in patients at risk for adverse cardiovascular outcomes, including age 65 years or older, current or previous long-term smokers, a history of cardiovascular disease, and a history of cancer 1.
• JAK inhibitors may be associated with higher risk of major adverse cardiovascular events and cancer than TNF antagonists in older adults with cardiovascular risk factors 1.
• Tofacitinib has restricted use in advanced therapy-naïve patients, and its use should be considered carefully in patients with a history of malignancy or severe organ dysfunction 1.

From the FDA Drug Label

INDICATIONS AND USAGE XELJANZ/XELJANZ XR/XELJANZ Oral Solution is a Janus kinase (JAK) inhibitor indicated for: • Rheumatoid Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers • Psoriatic Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers. • Ankylosing Spondylitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more TNF blockers. • Ulcerative Colitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to one or more TNF blockers • Polyarticular Course Juvenile Idiopathic Arthritis: XELJANZ/XELJANZ Oral Solution is indicated for the treatment of active polyarticular course juvenile idiopathic arthritis (pcJIA) in patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers

The use of Tofacitinib (Xeljanz) is for the treatment of:

• Rheumatoid Arthritis
• Psoriatic Arthritis
• Ankylosing Spondylitis
• Ulcerative Colitis
• Polyarticular Course Juvenile Idiopathic Arthritis 2

From the Research

Uses of Tofacitinib

• Tofacitinib is used for the treatment of rheumatoid arthritis (RA) as an oral Janus kinase inhibitor 3.
• It is also used for the induction and maintenance of remission in ulcerative colitis, particularly in cases of biological failure or steroid-dependent and thiopurine refractory disease 4, 5.
• The typical induction dose for ulcerative colitis is 10 mg twice daily, with a possible reduction to 5 mg twice daily in patients who respond to treatment 4.

Administration and Dosage

• For rheumatoid arthritis, tofacitinib can be administered as monotherapy or in combination with methotrexate, with doses ranging from 1-30 mg twice daily 3.
• A dose of 5 mg or 10 mg twice daily is commonly used for rheumatoid arthritis and ulcerative colitis 3, 6, 4.

Precautions and Safety Considerations

• Tofacitinib may increase the risk of infections, such as herpes zoster and tuberculosis, and should be used cautiously in patients with a history of these conditions 6, 4, 7.
• Patients with cardiovascular risk factors, previous thrombotic episodes, or a history of malignancy should be carefully evaluated before starting tofacitinib 6, 4, 7.
• Baseline testing for hepatitis B infection and latent tuberculosis is recommended, as well as complete adult vaccination, including Herpes zoster, before starting tofacitinib 4.