What is tofacitinib?

Tofacitinib (brand name: Xeljanz®) is a tablet that belongs to a class of medicines called Janus Kinase (JAK) inhibitors. JAK inhibitors work by blocking signals involved in inflammation. Blocking these signals in rheumatoid arthritis reduces pain, stiffness, swelling and damage in the joints.

What benefit can you expect from your treatment?

You may notice some relief of joint swelling, pain and stiffness within the first 2 to 4 weeks of treatment, though it can take up to 3 months to improve.

Stopping tofacitinib

If you stop or delay your tofacitinib treatment, your disease may get worse. Keep taking your treatment, unless advised by your rheumatologist to stop or unless serious side effects occur (see Side effects).

If you stop tofacitinib for any reason you must contact your rheumatologist. Failure to do so may mean that your treatment may no longer be subsidised.

How will your condition be monitored?

• Medicines like tofacitinib are very expensive and are highly funded by Medicare. Certain conditions must be met to receive it.
• Tofacitinib will only be given if your disease is active and if standard treatments have not worked.
• It will only be kept going if it helps your condition. This will be checked around 12 weeks after the start of treatment.
• Blood tests are needed during your treatment to watch for side effects and to decide if the treatment is working.
• How often you have blood tests will depend on what other medicines you are taking and what other illnesses you have. Your rheumatologist will advise on this.

How is tofacitinib taken?

Tofacitinib is taken by mouth in tablet form. The tablet should be swallowed whole do not crush or break the tablet.

When should it be taken?

• Take this medicine with a full glass of water at the same time each day. It can be taken with or without food.

If you miss a dose

• Take a dose as soon as you remember. If it is almost time for your next dose, wait until then and take a regular dose. Do not take extra medicine to make up for a missed dose.

What is the dosage?

• The usual dose for adults with rheumatoid arthritis is one 5mg tablet taken orally twice daily.

Can other medicines be taken with tofacitinib?

Tofacitinib may be used alone or with other arthritis medicines including:

• other disease modifying anti rheumatic drugs (DMARDs) such as methotrexate;
• steroid medicines such as prednisolone or cortisone injections into the joint;
• anti-inflammatory medicines (NSAIDs) such as naproxen (Naprosyn®) or ibuprofen (Brufen®, Nurofen®);
• simple pain medicines such as paracetamol.

Tofacitinib cannot be used with other biologic DMARDs or targeted synthetic DMARDs (such as baricitinib).

Are there any side effects?

You might experience side effects with your treatment. Tell your doctor if you notice side effects that you think are caused by this medicine. Many side effects disappear when tofacitinib treatment is stopped.

Most common side effects

• The most common side effects reported are mild upper respiratory tract infections (common cold, sinus infections), nausea, cough, and fever. Infections may need treatment and tofacitinib may need to be stopped for a while if you develop infection, so it is important to contact your doctor for advice

Less common or rare side effects

• Blood clots in the veins of the legs or lungs and arteries are possible in some people taking tofacitinib. This can happen more often in patients with an inflammatory condition. Further risk factors including heart disease will be assessed by your doctor.
• Serious infections such as tuberculosis (TB) are seen rarely, and screening for TB is needed before treatment begins.
• Increases in lipid (cholesterol) levels have been noted in some patients when taking tofacitinib and will be checked using blood tests.
• Changes in liver function have been seen. It is recommended to have regular liver function tests.
• Tofacitinib increases the risk of getting shingles. If you get a painful skin rash with blisters inform your doctor immediately. Vaccination for shingles should be discussed with your rheumatologist before starting treatment.
• Tofacitinib may increase the chance of bowel perforation, though this is rare.
• People with rheumatoid arthritis are at increased risk of lymphoma and some other cancers. Medicines that change your immune system like tofacitinib may increase this risk.
• Skin cancers have been reported in people taking tofacitinib and yearly skin checks are recommended.
• Tell your doctor or pharmacist immediately of any of side effects you experience.

What precautions are necessary

Infections

• If you have an active infection of any kind, treatment with tofacitinib will not be started until the infection is treated successfully.

Precautions with other diseases

• Tofacitinib should be used with caution in patients with slow heart rates (slow pulse) and who use medications that can cause heart block. Care should be taken in patients with a history of angina, heart attack or heart failure.
• The dose of your medication may need to be adjusted if you have kidney or liver disease.
• Sometimes tofacitinib may cause an ulcer in your stomach or gut, especially if this has been a problem in the past. Tell your doctor straight away if you have stomach ache or pain that won't go away or a change in bowel habits.

Use with other medicines

• Some medicines can affect tofacitinib or may affect how well it works. It is noted to interact with anti-fungal therapy such as ketoconazole, some antibiotics such as rifampicin and some heart medicines
• You should tell all your doctors about all medicines you are taking or plan to take. This includes all over the counter, herbal/naturopathic treatments.

Vaccines

• If you are taking tofacitinib you should not be immunised with ‘live’ vaccines such as: MMR (measles, mumps and rubella), OPV (oral polio virus), varicella vaccines (Chicken Pox/shingles), Japanese Encephalitis, BCG (Bacillus Calmette-Guerin) or Yellow Fever. Talk with your rheumatologist before receiving any vaccines.
• Pneumococcal vaccines and the yearly seasonal flu vaccinations are encouraged

For more information on vaccination including the COVID-19 vaccination go to the Vaccinations page on the ARA website

Surgery

• If you require surgery for any reason, treatment wJunith tofacitinib should be stopped one week before surgery. It will be restarted again after the operation at a time agreed by your surgeon and rheumatologist (usually when the wound is healed).

Use in pregnancy and when breastfeeding

• It is important to discuss with you doctor if you are planning a pregnancy while on tofacitinib.
• Tofacitinib should not be used during pregnancy. Women of childbearing potential should use effective birth control both during treatment and for at least 4 weeks after final dose of tofacitinib.
• Do not breastfeed if you are taking tofacitinib as it is uncertain how much of the drug might be excreted in breastmilk.

More information on pregnancy is available here.

How to store tofacitinib

• Store tofacitinib in a cool, dry place, away from direct heat and light (e.g., not in the bathroom).
• Keep all medicines out of reach of children.

Important things to remember

• You must see your rheumatologist regularly to ensure the treatment is working and minimise any possible side effects.
• You should have regular blood tests as suggested by your rheumatologist.
• It is important to tell your rheumatologist if you have a new serious illness such as a serious infection, cancer or heart failure.
• If you are worried about any side effects you should contact your rheumatologist as soon as possible.
• If you stop tofacitinib for any reason, you must contact your rheumatologist. Failure to do so may mean that your treatment may no longer be funded.
• If you are taking tofacitinib and plan to become pregnant you must discuss the timing with your rheumatologist.

The information  in this sheet has been obtained from various sources and have been reviewed by the Australian Rheumatology Association (ARA). It is intended as an educational aid and does not cover all possible uses, actions, precautions, side effects, or interactions of the medicines mentioned. This information is not intended as medical advice for individual problems nor for making an individual assessment of the risks and benefits of taking a particular medicine. It can be reproduced in its entirety but cannot be altered without permission from the ARA. The NHMRC publication: How to present the evidence for consumers: preparation of consumer publications (2000) was used as a guide in developing this publication.

Last reviewed June 2021.