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Medications > Tofacitinib | Xeljanz > Tofacitinib (Xeljanz) – Detailed Information

Tofacitinib (Xeljanz®)

What is Tofacitinib (Xeljanz)?

Tofacitinib (Xeljanz) is a Disease Modifying Anti-Rheumatic Drug (DMARD) first available in 2012. It is currently approved for the treatment of moderate to severe rheumatoid arthritis with or without methotrexate.  Tofacitinib is being studied for other types of arthritis (psoriatic) and  for diseases other than arthritis (Crohn’s disease & transplantation).

How does Tofacitinib (Xeljanz) work?

Cells in our body talk with each other. One way of doing this is through special proteins called cytokines. Cytokines are made and released by cells. Cytokines then bind to receptors on the surface of other cells. This results in a message being sent from the cell surface to the nucleus of the cell (called signal transduction). This signal results in the production of a protein or peptide by the DNA (activation of transcription).

One of the important signal transduction pathways in the body uses an enzyme called Janus Kinase (JAK) and another molecule called Signal Transducer and Activation of Transcription (STAT). The JAK-STAT pathway is important for sending signals involving bone marrow and immune system activation.

Tofacitinib is a new small molecule that enters a cell and binds to the ATP binding site on the enzyme Janus Kinase (JAK). By doing this it prevents JAK from activating STAT and sending the important message to the nucleus of the cell.

With rheumatoid arthritis the immune system is not functioning correctly. This causes an immune attack on the joints. Tofacitinib (Xeljanz) interferes with the immune system cells ability to talk with each other. When cells can’t talk they have a hard time co-ordinating their attack on the joints. The end result is improvement in the arthritis.

Why am I taking Tofacitinib (Xeljanz)?

Your doctor has prescribed this medicine to help with the following:

  • Reduce the pain and swelling (inflammation) in your joints.
  • Improve your day to day function.
  • Delay any long-term damage from the joint inflammation.

What is the usual dose of Tofacitinib (Xeljanz)?

  • Tofacitinib (Xeljanz) is taken by mouth (tablets)
  • Tofacitinib (Xeljanz) is available in 5 mg tablets
  • The standard dose is 5 mg (one tablet) twice a day

How often do I take Tofacitinib (Xeljanz)?

Tofacitinib (Xeljanz) is taken TWICE A DAY.

Who should NOT take Tofacitinib (Xeljanz)?

  • Patients who have had a previous reaction to tofacitinib.
  • Women who are pregnant, planning on becoming pregnant, or are breast feeding.
  • Some patients with diseases of the liver, kidney, or blood disorders.
  • Possibly patients who have cancer or have had a past history of certain cancers.
  • Patients with active infections.
  • Patients with a past history of tuberculosis.

When will I start to feel the effects of Tofacitinib (Xeljanz)?

Tofacitinib (Xeljanz) does not work right away.  It can take about 2 to 8 weeks before you start feeling better.  The maximum effect can take up to 3 – 6 months.  If your doctor changes the dose it can take another 2 to 8 weeks before you feel the effects.

What should I Avoid while taking Tofacitinib (Xeljanz)?

  • Do not get pregnant.
  • Do not take live vaccines (click here for a list of live vaccines).
  • If you are scheduled for surgery, let your doctor know.
  • Some medications may not be safe to take with tofacitinib (Xeljanz) including ketoconazole, fluconazole, and rifampin. Please discuss all new medications with your doctor.
  • Some medications may increase your risk of infection and should not be taken with tofacitinib (Xeljanz) including biologics and other potent immunosuppressives (i.e. cyclosporine & azathioprine). Please discuss with your doctor.

When should I NOT TAKE my Tofacitinib (Xeljanz)?

You should contact your doctor before missing a dose of tofacitinib (Xeljanz). However, in the following situations, it would be advisable to stop the tofacitinib (Xeljanz):

  • If you have a fever.
  • If you have or think you have an infection.
  • If you think you are pregnant.

Which Medications are safe to take with Tofacitinib (Xeljanz)?

Your rheumatologist may decide to add other medications to treat your arthritis. Tofacitinib (Xeljanz) can be safely taken with methotrexate.

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

LESS SERIOUS side-effects include:

  • Nausea, indigestion, and diarrhea.
  • Headaches
  • Upper respiratory tract infection (nasopharyngitis)
  • Cholesterol Levels – Tofacitinib (Xeljanz) may increase cholesterol levels. This will be monitored through blood tests.

MORE SERIOUS side-effects include:

  • Infection – There have been serious and rare infections associated with the use of tofacitinib (Xeljanz). Any infections or fevers should be taken very seriously and reviewed by your doctor.
  • Blood Counts – Tofacitinib (Xeljanz) can cause changes in the numbers of white blood cells (which are needed to fight infection) and red blood cells (which carry oxygen).
  • Liver – Tofacitinib may irritate the liver.  This does not usually cause symptoms but may be found on blood tests.  It is uncommon and usually reversible when regularly monitored with your monthly blood tests.
  • Bowels – Tofacitinib (Xeljanz) may increase the risk of bowel perforation.
  • Kidneys – Tofacitinib (Xeljanz) may cause a slight decrease in kidney function in some people (increased creatinine). This will be monitored through regular blood tests.

How can I help to minimize the side-effects of Tofacitinib (Xeljanz)?

  • Take your tofacitinib (Xeljanz) twice a day as prescribed by your doctor.
  • Get your blood tested regularly as directed by your doctor.
  • Attend your doctor’s appointments.

Do I need to have regular blood tests while taking Tofacitinib (Xeljanz)?

You will need BLOOD TESTS EVERY 1 – 3 MONTHS.  This is important to make sure the tofacitinib (Xeljanz) is having no harmful effects on your blood counts, liver, kidneys, or cholesterol levels.

How do I stop Tofacitinib (Xeljanz)?

You do not need to wean yourself off tofacitinib (Xeljanz).  It can simply be stopped.  However, your arthritis may “flare” after you stop the medicine.

Is Tofacitinib (Xeljanz) safe in pregnancy?

  • Tofacitinib (Xeljanz) may cause birth defects and result in miscarriage.  You should AVOID PREGNANCY while on tofacitinib (Xeljanz).
  • All women of child bearing potential taking tofacitinib (Xeljanz) must use reliable contraception.  If you become pregnant while taking tofacitinib (Xeljanz) NOTIFY YOUR DOCTOR IMMEDIATELY.
  • Do not breast feed while taking tofacitinib (Xeljanz).