Xeljanz XR

Dosage Forms & Strengths

tablet (Xeljanz)

• 5mg

tablet, extended-release (Xeljanz XR)

• 11mg

Rheumatoid Arthritis

Indicated as second-line treatment for moderate-to-severe active rheumatoid arthritis in patients with an inadequate response or intolerance to methotrexate; may be used as monotherapy or in combination with methotrexate or other nonbiologic DMARDs

5 mg PO BID or 11 mg PO qDay

Dosage Modifications

Coadministration with strong CYP3A4 inhibitors: Not to exceed 5 mg qDay

Coadministration with 1 or more drugs that result in both moderate CYP3A4 inhibition and strong CYP2C19 inhibition (eg, fluconazole): Not to exceed 5 mg qDay

Coadministration with strong CYP3A4 inducers: May result in loss of or reduced clinical response; coadministration is not recommended

Coadministration with methotrexate: No dosage adjustment required

Coadministration with P-gp inhibitors: No dosage adjustment required

Renal impairment

• Mild: No dosage adjustment required
• Moderate-to-severe: Not to exceed 5 mg qDay

Hepatic impairment

• Mild: No dosage adjustment required
• Moderate: Not to exceed 5 mg qDay
• Severe: Not recommended

Serious infection

• Interrupt treatment if serious infection develops until infection is controlled
• Lymphocytes ≥500/mm³: Maintain dose
• Lymphocytes <500/mm³: Discontinue until infection controlled

Neutropenia

• ANC >1000/mm³: Maintain dose
• ANC 500-1000/mm³: Interrupt dosing for persistent decreases; when ANC >1000/mm³, resume dose at 5 mg BID
• ANC <500/mm³: Discontinue

Anemia

• Hgb ≤2 g/dL decrease and level ≥9.0 g/dL: Maintain dose
• Hgb >2g/dL decrease or level <8.0 g/dL: Interrupt treatment until Hgb levels have normalized

Dosing Considerations

Should not be used in combination with biologic DMARDs or potent immunosuppressive agents (eg, azathioprine, cyclosporine)

Structural joint damage progression

• Radiographic response data from the ORAL Scan and ORAL Start studies evaluated the efficacy of tofacitinib on structural joint damage progression as measured by mean change from baseline in van der Heijde modified Total Sharp Score (mTSS) and its components, erosion score, and joint space narrowing (JSN) score
• In ORAL Scan, 74% of patients in the placebo/methotrexate group experienced no radiographic progression at Month 6 compared to 84% of patients treated with tofacitinib 5mg BID plus methotrexate
• In ORAL Start, 55% of patients in the methotrexate group experienced no radiographic progression at Month 6 compared to 73% of patients treated with tofactinib 5mg BID

Safety and efficacy not established

Before you start treatment with tofacitinib, your doctor may perform tests to make sure you do not have tuberculosis or other infections.

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

You may take tofacitinib with or without food.

Do not crush, chew, or break an extended-release tablet. Swallow it whole.

Tofacitinib can lower blood cells that help your body fight infections and help your blood to clot. Your blood will need to be tested often. Further doses may be delayed based on the results of these tests. Your doctor may also want to check your skin for signs of cancer.

If you have hepatitis B or C you may develop liver symptoms while taking this medicine. Your doctor may want to check your liver function before and during your treatment with tofacitinib.

Store in the original container at room temperature away from moisture and heat.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Many drugs can interact with tofacitinib. Not all possible interactions are listed here. Tell your doctor about all your medications and any you start or stop using during treatment with tofacitinib, especially:

• aprepitant, bosentan, haloperidol, imatinib, St. John's wort, ticlopidine;

• an antibiotic--ciprofloxacin, doxycycline, erythromycin, metronidazole, norfloxacin, tetracycline;

• an antidepressant--desipramine, fluoxetine, sertraline;

• antifungal medicine--clotrimazole, fluconazole, voriconazole;

• heart or blood pressure medicine--amiodarone, diltiazem, dronedarone, lidocaine, verapamil;

• HIV/AIDS medication--atazanavir, efavirenz, darunavir when given with ritonavir, fosamprenavir, nevirapine, saquinavir;

• medicines to prevent organ transplant rejection--azathioprine, cyclosporine, tacrolimus;

• other arthritis medicines--abatacept, adalimumab, anakinra, certolizumab, etanercept, golimumab, infliximab, rituximab, tocilizumab;

• seizure medicine--carbamazepine, fosphenytoin, oxcarbazepine, phenobarbital, phenytoin, primidone;

• a stomach acid-reducer--cimetidine, esomeprazole, omeprazole; or

• tuberculosis medicine--rifabutin, rifampin, rifapentine.

This list is not complete and many other drugs can interact with tofacitinib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Give a list of all your medicines to any healthcare provider who treats you.

If you will be using this medicine for a long time, it is very important that your doctor check your progress at regular visits. This will allow your doctor to see if this medicine is working properly and to decide whether you should continue to use it. Blood tests may be needed to check for unwanted effects.

You will need to have a skin test for tuberculosis before you start using this medicine. Tell your doctor if you or anyone in your home has ever had a positive reaction to a tuberculosis skin test.

Your body's ability to fight infection may be reduced while you are using tofacitinib. It is very important that you call your doctor at the first sign of an infection. Check with your doctor right away if you have a fever, chills, cough, flu-like symptoms, or unusual tiredness or weakness.

Using this medicine may increase your risk of getting skin cancer (eg, non-melanoma skin cancer) or cancer of the lymph system (lymphoma). Talk to your doctor if you have concerns about this risk.

Tofacitinib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
• Check with your doctor immediately if you notice any unusual bleeding or bruising, black, tarry stools, blood in the urine or stools, or pinpoint red spots on your skin.
• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injury could occur.

While you are being treated with tofacitinib, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Tofacitinib may lower your body's resistance and the vaccine may not work as well or you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

• It is used to treat rheumatoid arthritis.

Use Xeljanz XR as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with or without food.
• Take as you have been told by your doctor.
• Swallow whole. Do not chew, break, or crush.

What do I do if I miss a dose?

• Skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache.
• Loose stools (diarrhea).
• Signs of a common cold.
• Runny nose.
• Sore throat.
• Stuffy nose.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• This medicine comes with an extra patient fact sheet called a Medication Guide. Read it with care. Read it again each time this medicine is refilled. If you have any questions about Xeljanz XR, please talk with the doctor, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about Xeljanz XR. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using Xeljanz XR (tofacitinib extended-release tablets).

Review Date: October 4, 2017