Generic name: tofacitinib (TOE fa SYE ti nib)
Brand name: Xeljanz, Xeljanz XR
Drug class: Antirheumatics
Xeljanz (tofacitinib) blocks the activity of certain enzymes in the body that affect immune system function.
Xeljanz is used to treat moderate to severe rheumatoid arthritis or active psoriatic arthritis in adults who have tried methotrexate or other medications without successful treatment of symptoms. Tofacitinib is sometimes given in combination with methotrexate or other arthritis medicines.
Xeljanz is used to treat adults with moderate to severe ulcerative colitis in adults who cannot use certain other medications, or after other treatments have failed.
Xeljanz is also used to treat active polyarticular juvenile arthritis in patients 2 years of age and older.
Warnings
You should not use Xeljanz if you have a serious infection. Before you start treatment, your doctor may perform tests to make sure you do not have an infection.
Tofacitinib affects your immune system. You may get infections more easily, even serious or fatal infections. Call your doctor if you have a fever, chills, aches, tiredness, cough, trouble breathing, skin sores, diarrhea, weight loss, or burning when you urinate.
If you've ever had hepatitis B or C, using Xeljanz can cause this virus to become active or get worse. Tell your doctor if you don't feel well and you have right-sided upper stomach pain, vomiting, loss of appetite, or yellowing of your skin or eyes.
Before taking this medicine
You should not use Xeljanz if you are allergic to tofacitinib, or if you have any kind of infection.
To make sure Xeljanz is safe for you, tell your doctor if you have ever had:
- liver disease (especially hepatitis B or C);
- heart problems (especially if you are 50 or older);
- lung disease;
- a blood clot;
- a chronic infection;
- HIV, or a weak immune system;
- a stomach or intestinal problem such as diverticulitis or an ulcer;
- kidney disease (or if you are on dialysis);
- diabetes; or
- if you are scheduled to receive any vaccine.
Taking Xeljanz at too high a dose may increase the risk of death in people with rheumatoid arthritis who are 50 and older and have at least 1 risk for heart disease. This includes high blood pressure, high cholesterol, diabetes, smoking, being overweight, or having a family history of heart disease. Talk to your doctor about your specific risk, and take only your recommended dose.
Tell your doctor if you have ever had tuberculosis or if anyone in your household has tuberculosis. Also tell your doctor if you have recently traveled. Tuberculosis and some fungal infections are more common in certain parts of the world, and you may have been exposed during travel.
Using Xeljanz may increase your risk of developing certain cancers, such as lymphoma or skin cancer. Ask your doctor about this risk.
It is not known whether tofacitinib will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. Tofacitinib may affect your ability to have children during treatment and in the future.
If you are pregnant, your name may be listed on a pregnancy registry to track the effects of tofacitinib on the baby.
Do not breastfeed while you are using Xeljanz, and for at least 18 hours after your last dose (36 hours if you take extended-release tablets). If you use a breast pump during this time, do not feed the milk to your baby.
Do not give Xeljanz to a child without medical advice. Xeljanz XR extended-release tablets are not approved for use by anyone younger than 18 years old.
How should I take Xeljanz?
Before you start treatment with Xeljanz, your doctor may perform tests to make sure you do not have tuberculosis or other infections.
Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.
A safe dose of Xeljanz is not the same for all conditions. Avoid medication errors by using only the form and strength your doctor prescribes.
Tofacitinib doses are based on weight in children and teenagers. Your child's dose needs may change if the child gains or loses weight.
You may take Xeljanz with or without food.
Do not crush, chew, or break an extended-release tablet. Swallow the tablet whole.
Measure liquid medicine carefully. Use the dosing syringe provided, or use a medicine dose-measuring device (not a kitchen spoon).
If you've ever had shingles (herpes zoster) or hepatitis B or C, using Xeljanz can cause these viruses to become active or get worse. You may need frequent liver function tests.
Your doctor will need to examine you on a regular basis.
Store this medicine in the original container at room temperature, away from moisture, heat, and light. Throw away any unused liquid medicine after 60 days.
Some tablets are made with a shell that is not absorbed or melted in the body. Part of this shell may appear in your stool. This is normal and will not make the medicine less effective.
Dosing information
Usual Adult Dose for Rheumatoid Arthritis:
As monotherapy or in combination with nonbiologic disease-modifying antirheumatic drugs:
-Immediate-release: 5 mg orally 2 times a day
-Extended-release: 11 mg orally once a day
Comments:
-Do not initiate this drug if absolute lymphocyte count is less than 500 cells/mm3, absolute neutrophil count (ANC) is less than 1000 cells/mm3, or hemoglobin is less than 9 g/dL.
-Patients treated with the 5 mg immediate-release 2 times a day may be switched to the 11-mg extended-release once a day the day following the last dose of 5 mg.
Use: For moderately to severely active rheumatoid arthritis (RA) in adult patients who have had an inadequate response or intolerance to methotrexate; it may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs)
Usual Adult Dose for Psoriatic Arthritis:
In combination with nonbiologic disease-modifying antirheumatic drugs:
-Immediate-release: 5 mg orally 2 times a day
-Extended-release: 11 mg orally once a day
Comments:
-Do not initiate this drug if absolute lymphocyte count is less than 500 cells/mm3, absolute neutrophil count (ANC) is less than 1000 cells/mm3, or hemoglobin is less than 9 g/dL.
-Patients treated with the 5 mg immediate-release 2 times a day may be switched to the 11-mg extended-release once a day the day following the last dose of 5 mg.
Use: For active psoriatic arthritis in adult patients who have had an inadequate response or intolerance to methotrexate or other DMARDs
Usual Adult Dose for Ulcerative Colitis:
-Induction: 10 mg orally 2 times a day for 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response; if needed, continue 10 mg 2 times a day for a maximum of 16 weeks; discontinue 10 mg 2 times a day after 16 weeks if adequate therapeutic response is not achieved
-Maintenance: 5 mg orally 2 times a day; limit use of 10 mg 2 times a day beyond induction for those with loss of response
Comments:
-Do not initiate this drug if absolute lymphocyte count is less than 500 cells/mm3, absolute neutrophil count (ANC) is less than 1000 cells/mm3, or hemoglobin is less than 9 g/dL.
-Patients treated with the 5 mg immediate-release 2 times a day may be switched to the 11-mg extended-release once a day the day following the last dose of 5 mg.
Use: For the treatment of adult patients with moderately to severely active
ulcerative colitis (UC) who have had an inadequate response or who are intolerant to TNF blockers
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
What to avoid
Do not receive a "live" vaccine while using Xeljanz, or you could develop a serious infection. Live vaccines include measles, mumps, rubella (MMR), polio, rotavirus, typhoid, yellow fever, varicella (chickenpox), and zoster (shingles).
Xeljanz side effects
Get emergency medical help if you have signs of an allergic reaction to Xeljanz: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Some people taking high dosages of Xeljanz have developed serious or fatal blood clots in the lungs. Stop taking tofacitinib and seek emergency medical attention if you have:
- sudden shortness of breath;
- pain while breathing;
- cough with pink or red mucus;
- pain in your chest or back;
- clammy or blue-colored skin, heavy sweating; or
- pain, swelling, or redness in an arm or a leg.
You may get infections more easily, even serious or fatal infections. Call your doctor right away if you have signs of infection such as:
- fever, chills, sweating, tiredness, muscle pain;
- feeling short of breath;
- skin sores with warmth, redness, or swelling;
- increased urination, pain or burning when you urinate;
- mouth sores, stomach pain, diarrhea; or
- signs of tuberculosis: fever, cough, night sweats, loss of appetite, weight loss, and feeling very tired.
Further doses may be delayed until your infection clears up.
Also call your doctor at once if you have:
- low red blood cells (anemia) - pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet;
- signs of hepatitis - loss of appetite, vomiting, stomach pain (upper right side), dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
- signs of shingles - -flu-like symptoms, tingly or painful blistering rash on one side of your body; or
- signs of perforation (a hole or tear) in your stomach or intestines - fever, ongoing stomach pain, change in bowel habits.
Common Xeljanz side effects may include:
- skin rash, shingles;
- increased blood pressure;
- abnormal blood tests;
- fever;
- headache;
- nausea, vomiting, diarrhea; or
- cold symptoms such as stuffy nose, sneezing, sore throat.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What other drugs will affect Xeljanz?
Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.
Tell your doctor about all your current medicines. Many drugs can interact with tofacitinib, especially:
- azathioprine;
- cyclosporine; or
- other drugs to treat arthritis or ulcerative colitis - abatacept, adalimumab, anakinra, certolizumab, etanercept, golimumab, infliximab, rituximab, secukinumab, tocilizumab, ustekinumab, vedolizumab.
This list is not complete and many other drugs may interact tofacitinib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.