Tofacitinib

Tofacitinib is a prescription medication used to treat rheumatoid arthritis in adult patients who have been treated with methotrexate without success.

Rheumatoid arthritis is a disease of the immune system. Tofacitinib belongs to a group of drugs called JAK inhibitors which work by suppressing the immune system against the damaging inflammation of rheumatoid arthritis.

This medication comes in tablet form and is taken once or twice daily, with or without food.

Common side effects of tofacitinib include runny or stuffy nose, headaches, and diarrhea.

Tofacitinib is a prescription medicine used to treat adults with moderately to severely active rheumatoid arthritis in which methotrexate did not work well.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Tofacitinib may be found in some form under the following brand names:

• Xeljanz

Tofacitinib may cause serious side effects. See "Precautions" section.

Common side effects of tofacitinib include:

• upper respiratory tract infections (common cold, sinus infections)
• headache
• diarrhea
• nasal congestion, sore throat, and runny nose (nasopharyngitis)　

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all the possible side effects of tofacitinib. For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Tofacitinib and other medicines may affect each other causing side effects.

Especially tell your healthcare provider if you take:

• any other medicines to treat your rheumatoid arthritis. You should not take tocilizumab (Actemra), etanercept (Enbrel), adalimumab (Humira), infliximab (Remicade), rituximab (Rituxan), abatacept (Orencia), anakinra (Kineret), certolizumab (Cimzia), golimumab (Simponi), azathioprine, cyclosporine, or other immunosuppressive drugs while you are taking tofacitinib. Taking tofacitinib with these medicines may increase your risk of infection.
• medicines that affect the way certain liver enzymes work. Ask your healthcare provider if you are not sure if your medicine is one of these.

Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Hepatitis B or C activation infection in people who carry the virus in their blood. Tell your healthcare provider if you have any of the following symptoms of a possible hepatitis B or C infection:

• feel very tired
• skin or eyes look yellow
• little or no appetite
• vomiting
• clay-colored bowel movements
• fevers
• chills
• stomach discomfort
• muscle aches
• dark urine
• skin rash

Serious infections. Tofacitinib can lower the ability of your immune system to fight infections. Some people have serious infections while taking tofacitinib, including tuberculosis (TB), and infections caused by bacteria, fungi, or viruses that can spread throughout the body. Some people have died from these infections.

• Your healthcare provider should test you for TB before starting tofacitinib.
• Your healthcare provider should monitor you closely for signs and symptoms of TB infection during treatment with tofacitinib.

You should not start taking tofacitinib if you have any kind of infection unless your healthcare provider tells you it is okay.

Before starting tofacitinib, tell your healthcare provider if you:

• think you have an infection or have symptoms of an infection such as:
  • fever, sweating, or chills
  • muscle aches 
  • cough 
  • shortness of breath 
  • blood in phlegm 
  • weight loss
  • warm, red, or painful skin or sores on your body 
  • diarrhea or stomach pain 
  • burning when you urinate or urinating more often than normal 
  • feeling very tired
• are being treated for an infection
• get a lot of infections or have infections that keep coming back
• have diabetes, HIV, or a weak immune system. People with these conditions have a higher chance for infections.
• have TB, or have been in close contact with someone with TB
• live or have lived, or have traveled to certain parts of the country (such as the Ohio and Mississippi River valleys and the Southwest) where there is an increased chance for getting certain kinds of fungal infections (histoplasmosis, coccidioidomycosis, or blastomycosis). These infections may happen or become more severe if you use tofacitinib. Ask your healthcare provider if you do not know if you have lived in an area where these infections are common.
• have or have had hepatitis B or C

Cancer and immune system problems. Tofacitinib may increase your risk of certain cancers by changing the way your immune system works.

• Lymphoma and other cancers can happen in patients taking tofacitinib. Tell your healthcare provider if you have ever had any type of cancer.
• Some people who have taken tofacitinib with certain other medicines to prevent kidney transplant rejection have had a problem with certain white blood cells growing out of control (Epstein Barr Virus-associated post transplant lymphoproliferative disorder).

Tears (perforation) in the stomach or intestines. Tell your healthcare provider if you have had diverticulitis (inflammation in parts of the large intestine) or ulcers in your stomach or intestines. Some people taking tofacitinib get tears in their stomach or intestine. This happens most often in people who also take nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, or methotrexate.

• Tell your healthcare provider right away if you have fever and stomach-area pain that does not go away, and a change in your bowel habits.

Changes in certain laboratory test results. Your healthcare provider should do blood tests before you start receiving tofacitinib and while you take tofacitinib to check for the following side effects:

• changes in lymphocyte counts. Lymphocytes are white blood cells that help the body fight off infections.
• low neutrophil counts. Neutrophils are white blood cells that help the body fight off infections.
• low red blood cell count. This may mean that you have anemia, which may make you feel weak and tired.

Your healthcare provider should routinely check certain liver tests.

You should not receive tofacitinib if your lymphocyte count, neutrophil count, or red blood cell count is too low or your liver tests are too high.

Your healthcare provider may stop your tofacitinib treatment for a period of time if needed because of changes in these blood test results.

You may also have changes in other laboratory tests, such as your blood cholesterol levels.

Your healthcare provider should do blood tests to check your cholesterol levels 4 to 8 weeks after you start receiving tofacitinib, and as needed after that. Normal cholesterol levels are important to good heart health.

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of tofacitinib there are no specific foods that you must exclude from your diet when receiving tofacitinib.

Before taking tofacitinib, tell your healthcare provider if you:

• have an infection. See "Drug Precautions" section.
• have liver problems
• have kidney problems
• have any stomach area (abdominal) pain or been diagnosed with diverticulitis or ulcers in your stomach or intestines
• have had a reaction to tofacitinib or any of the ingredients in tofacitinib
• have recently received or are scheduled to receive a vaccine. People who take tofacitinib should not receive live vaccines. People taking tofacitinib can receive non-live vaccines.
• have any other medical conditions
• plan to become pregnant or are pregnant. It is not known if tofacitinib will harm an unborn baby.
• plan to breastfeed or are breastfeeding. You and your healthcare provider should decide if you will take tofacitinib or breastfeed. You should not do both.

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

There is a registry for pregnant women who are taking this medication. The purpose of this registry is to check the health of the pregnant mother and her baby. If you are pregnant or become pregnant while taking tofacitinib, talk to your healthcare provider about how you can join this pregnancy registry or you may contact the registry at 1-877-311-8972 to enroll.

Tell your healthcare provider if you plan to breastfeed or are breastfeeding. You and your healthcare provider should decide if you will take tofacitinib or breastfeed. You should not do both.

Take tofacitinib as your healthcare provider tells you to take it.

• Take tofacitinib 2 times a day with or without food.
• If you take too much tofacitinib, call your healthcare provider or go to the nearest hospital emergency room right away.

Tofacitinib may be used alone or in combination with other medications. The recommended dose of tofacitinib is 5 mg twice daily. Your healthcare provider may reduce your dose or interrupt therapy if you have kidney or liver disease and certain other conditions or if you are experiencing serious side effects.

If you take too much tofacitinib, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
 

• Store tofacitinib at 68°F to 77°F (room temperature).
• Safely throw away medicine that is out of date or no longer needed.
• Keep tofacitinib and all medicines out of the reach of children.

WARNING: SERIOUS INFECTIONS AND MALIGNANCY

SERIOUS INFECTIONS

Patients treated with tofacitinib are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids.

If a serious infection develops, interrupt tofacitinib until the infection is controlled.

Reported infections include:

1. Active tuberculosis, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent tuberculosis before tofacitinib use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib use.
2. Invasive fungal infections, including cryptococcosis and pneumocystosis. Patients with invasive fungal infections may present with disseminated, rather than localized, disease.
3. Bacterial, viral, and other infections due to opportunistic pathogens.

The risks and benefits of treatment with tofacitinib should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection.

Patients should be closely monitored for the development of signs and symptoms of infection during and after treatment with tofacitinib, including the possible development of tuberculosis in patients who tested negative for latent tuberculosis infection prior to initiating therapy.

MALIGNANCIES

Lymphoma and other malignancies have been observed in patients treated with tofacitinib. Epstein Barr Virus- associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with tofacitinib and concomitant immunosuppressive medications