Tofacitinib is a small molecule drug, which means that it’s less likely to stop working over time than biologic medicines such as infliximab, adalimumab, golimumab or vedolizumab. Biologics are larger molecules that the immune system sometimes recognises as a foreign substance and thinks is harmful. It then produces proteins called antibodies to the biologic medicine and these prevent it from working as well.

If your condition hasn’t changed after the first eight weeks, your IBD team may decide to continue with the medication for a further eight weeks. But if treatment hasn’t worked for you after this time (16 weeks in total), it should be stopped as it’s not the right treatment for you. Your IBD team will talk to you about the other options available.

• one tablet in the morning
• one tablet in the evening

Try to take your tablets at a similar time every day. You can take it with or without food, and if you have difficulty swallowing the tablet, it can be crushed and taken with water.

If your Ulcerative Colitis flares whilst on 5mg twice a day, your dose can be increased back to 10mg twice a day to try to reduce the inflammation and symptoms. However there is a higher risk of side effects on the 10mg dose.

If you’re taking mesalazine you can stay on this whilst taking tofacitinib.

But you shouldn’t be prescribed tofacitinib with a biologic medicine such as infliximab, adalimumab, golimumab, vedolizumab or immunosuppressants such as azathioprine, methotrexate or mercaptopurine. If you are taking any of these medications, it is important that you stop them before starting tofacitinib.

Medicines that contain any of the following may also affect how the tofacitinib works:

• antibiotics used to treat bacterial infections such as clarithromycin and rifampicin.
• antifungals used to treat fungal infections such as fluconazole, ketoconazole, clotrimazole, itraconazole, and voriconazole.

This isn’t a full list so talk to your IBD team or pharmacist before you take any other medicines.

You’ll have blood tests to check your full blood count, kidney function and lipids. Your IBD team may want to check if you’ve been exposed to a variety of viral infections including HIV, Hepatitis B and C, EBV (Epstein-Barr virus) and varicella to ensure that it is a safe and appropriate. They will also screen for tuberculosis.

Vaccinations

Tofacitinib acts on the immune system and can make you more susceptible to infections. It can also cause previous viral infections, such as shingles, to return. To reduce this risk, you should have all the vaccinations you need before you start treatment.

If these are “live” vaccines such as the varicella zoster vaccination for shingles, you’ll need to have this at least two weeks and ideally four weeks before you start the tofacitinib. 

Make sure your IBD team know if you have a history of:

Tuberculosis. If you have any history of tuberculosis (TB) or any recent exposure to people with TB. You should not be given tofacitinib if you have active TB, and if you have underlying, inactive TB, this will need to be treated before you start therapy. Most doctors now use a blood test to check for underlying or inactive TB, but you may be given a chest x-ray as well.

Infections. If you have a history of infections or currently have an infection, such as tonsillitis or a urinary tract infection, or have symptoms such as feeling feverish or generally unwell. Your tofacitinib treatment may need to be postponed until the any infection has cleared. This is because taking tofacitinib could make the infection worse.

Heart problems. If you have heart problems such as congestive heart failure, ischemic heart disease or a history of fainting, tofacitinib may make your symptoms worse.

Heart problems. Tofacitinib has been associated with an increased risk of heart problems, including heart attacks. This risk increases with age and is higher in people who smoke, those with diabetes and people who already have heart disease¹¹. Tell your doctor if you have heart problems, high blood pressure, high cholesterol or if you have ever smoked. If your IBD team think that you are at increased risk of heart attacks, they may decide that tofacitinib is not right for you.

Blood clots. Tofacitinib may increase the risk of blood clots in the legs (deep vein thrombosis) or lungs (pulmonary embolism). If you have a history of previous blood clots this medication is not right for you and you will not be offered this.

Cancer. Tofacitinib has been associated with an increased risk of some cancers. This risk increases with age and is higher in people who smoke and who have or have previously had cancer. Tell your doctor if you have ever had any type of cancer or if you have ever smoked. If your IBD team think that you are at increased risk of cancer, they may decide that tofacitinib is not right for you.

Liver problems. If you’ve previously had hepatitis you may need regular checks for this as tofacitinib may increase the risk of you having hepatitis again.

Your doctor will give you a Patient Alert Card which contains important information about what to look out for.

To reduce risks:

• Have the annual flu vaccination. You may also be advised to have a pneumonia vaccination. If left untreated pneumococcal infections can lead to pneumonia (inflammation of tissue in the lungs) septicaemia (a kind of blood poisoning) and meningitis (an infection of the protective membranes that surround the brain and spinal cord).
   
• Try to avoid close contact with people who have infections. This includes viruses and bacteria that cause chickenpox and shingles, measles, and pneumococcal disease. Contact your IBD team or doctor if you begin to feel unwell and think you may have caught an infection.
   
• Take care in the sun. There is a small increased risk of skin cancers for people who take tofacitinib. Take precautions in the sun including using sunblock, wearing a hat, covering your skin when you are out in strong sunshine and don’t use sun beds.

Some of the most common side effects are mentioned below. You can find a full list in the Patient Information Leaflet (PIL) that comes with your medicine or at www.medicines.org.uk.

Immediate reactions

Any medication can cause an allergic reaction. Tell your doctor immediately if you develop any of the following symptoms:

• difficulty breathing or swallowing
• rash, hives (swollen red patches of skin) or other signs of allergic reaction
• swollen face including lips and mouth or hands and feet
  
  

Common side effects

The most common side effects that people experience when are taking tofacitinib are headache, runny or stuffy nose and slight swelling at the back of the throat (nasopharyngitis), feeling sick (nausea) and joint pain (arthralgia).

Other side effects

Because tofacitinib acts on the immune system it can have some serious side effects. Your IBD team will continue to monitor you to minimise risks but let them know if you:

• think you have an infection including having a fever, sore throat and achiness.
• have a bump or open sore which is not healing.
• have gut symptoms that are not improving or are getting worse, especially if you also have a fever. There may also be a risk of gut perforation.

There is an increased risk of shingles (herpes zoster reactivation). If you develop blister like skin eruptions or a painful rash you should stop the medication immediately and contact your IBD team. You can normally restart the drug once the rash has healed.

Tofacitinib may increase the risk of blood clots in your legs (deep vein thrombosis) or lungs (pulmonary embolism). Seek urgent medical care if you develop swelling of your legs or arms with reddened and swollen skin. Or breathlessness, difficulty breathing, chest or back pain whilst you’re on this medication.

Tofacitinib may increase the risk of a heart attack. Seek urgent medical care if you develop severe chest pain or tightness (that may spread to arms, jaw, neck and back), shortness of breath, cold sweats, light headedness or sudden dizziness.

Tofacitinib may raise levels of blood cholesterol in some people. Your IBD team will monitor this with regular blood tests.

Some people taking tofacitinib may be at increased risk of fractures. This risk increases with age and is likely to be higher people who have had a fracture or who have osteoporosis, in women and people taking steroids. If you have osteoporosis or are concerned about this risk discuss it with your IBD team.

If you are worried about any new or ongoing symptoms talk to your IBD team. 

In the UK, live vaccines include:

• Rotavirus vaccine.
• Measles, mumps and rubella (MMR) vaccine.
• Nasal flu vaccine used in children: the injected flu vaccine used in adults is not
• Shingles vaccine: a non-live vaccine is also available for people with severe immunosuppression.
• Chickenpox vaccine.
• BCG vaccine against TB.
• Yellow fever vaccine.
• Oral typhoid vaccine: but the injected typhoid vaccine is not live

You can use oral contraception when you’re taking tofacitinib. Our information sheet on Reproductive Health can help you decide on the right contraceptive for you based on your Colitis symptoms.

If you do become pregnant whilst you’re taking tofacitinib

Tell your IBD team immediately. There are reports of some women who have become pregnant while taking tofacitinib, mostly in early pregnancy. In these women there wasn’t any increase in miscarriage or birth defects in the baby.

If you are planning to become pregnant

We don’t know yet if tofacitinib affects fertility in men or women. If you’re planning to get pregnant tell your IBD team as you will need to stop taking tofacitinib.

What about breastfeeding?

It’s not yet known whether tofacitinib is present in breast milk so as a precaution you should avoid breastfeeding.

Tofacitinib stops working

Because tofacitinib is a small molecule, antibodies to the drug are not likely to form. This means that tofacitinib is less likely than biologics to stop working over time. But if it does stop working you can increase the dose back to 10mg twice daily to recapture the previous benefit, although this does increase the risk of side effects. If you stop the drug for a period of time it can be re-started later without an increased risk of side effects or lack of response.

Side effects

If side effects are serious or difficult to manage, your IBD team will talk to you about your options.

Your IBD team should give you clear information, talk with you about your options and listen carefully to your views and any worries or concerns you may have. The choice of treatment between tofacitinib, biological drugs and surgery should be made after talking with your IBD team about the possible advantages and disadvantages of all the options. You can also talk to the Crohn’s & Colitis UK Helpline.