Xeljanz (Tofacitinib)

How does Xeljanz (Tofacitinib) work?

Xeljanz belongs to the drug class Janus kinase (JAK) inhibitors. It works by blocking the action of Janus kinase enzymes, which cause the inflammation seen in patients with rheumatoid arthritis, active psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and juvenile idiopathic arthritis.

How it’s Used?

Storage

Xeljanz should be stored at room temperature between 68°F to 77°F (20°C to 25°C).

How to Take

Xeljanz tablets should be swallowed whole. Do not crush, chew or break extended-release tablets.

Dosage

Xeljanz is available in immediate-release tablets, extended-release tablets, and an oral solution.

• Xeljanz immediate-release tablets are available in 5mg and 10mg tablets.
• Xeljanz extended-release tablets are available in 11mg and 22mg tablets.
• Xeljanz oral solution is available in 1mg/ml liquid.

Dosing for Adults

Rheumatoid Arthritis

The recommended starting dose of Xeljanz for the treatment of rheumatoid arthritis is

• Immediate-release tablets: 5mg twice daily
• Extended-release tablets 11mg once daily

Psoriatic arthritis

The recommended starting dose of Xeljanz for the treatment of psoriatic arthritis is

• Immediate-release tablets: 5mg twice daily
• Extended-release tablets 11mg once daily

Ankylosing Spondylitis

The recommended starting dose of Xeljanz for the treatment of ankylosing spondylitis is

• Immediate-release tablets: 5mg twice daily
• Extended-release tablets 11mg once daily

Ulcerative Colitis

The recommended starting dose of immediate-release tablets is 10mg twice daily and extended-release tablets 22mg daily for eight weeks. If remission is not achieved, this dose can be continued for a maximum of 16 weeks.

After 8 to 16 weeks, maintenance dosing should be dosed at immediate-release tablets of 5mg twice daily or extended-release tablets of 11mg.

Dosing for Children

Polyarticular Course Juvenile Idiopathic Arthritis

The recommended starting dose of Xeljanz for treating polyarticular course juvenile idiopathic arthritis is based on the child’s body weight. Children under 18 should only be prescribed immediate-release tablets or oral solution.

• Children 10kg-20kg: 3.2mg twice daily
• Children 20kg-40kg: 4mg twice daily
• Children >40kg: 5mg twice daily

Missed Dose

If you miss a dose of Xeljanz, take it as soon as you remember. If it’s almost time for your next dose, skip the missed dose and return to your regular schedule. Do not take two doses at the same time.

Overdose

Taking too much Xeljanz can lead to serious side effects. If you suspect an overdose, seek emergency medical attention or call the poison control helpline at 1-800-222-1222.

Side Effects

If you experience signs and symptoms of an allergic reaction, such as hives, rash, itching, difficulty breathing, or swelling of the face, mouth, or throat, seek medical attention immediately.

The most common side effects of Xeljanz include:

• Skin rashes (shingles have been reported)
• Increased blood pressure
• Fever
• Abnormal blood tests
• Headache
• Nausea, vomiting, and diarrhea
• Cold symptoms include a stuffy nose, sneezing, and sore throat.

Some serious side effects can also occur; seek immediate medical attention if you experience any of the following symptoms:

• Fever, chills, night sweats, fatigue
• Wheezing, trouble breathing, severe cough
• Pain while urinating
• Unexplained weight loss
• Lumps in the armpits, groin, or neck
• Sudden shortness of breath
• Chest pain/pressure
• Nausea, vomiting, cold sweats
• Lightheadedness like you may pass out
• Weakness on one side of the body, slurred speech, or drooping of one side of the face
• Pain, swelling, or redness in an arm or leg
• Severe abdominal pain with fever or bowel changes

Warnings & Precautions

Children

Xeljanz is approved for children two and older to manage polyarticular course juvenile idiopathic arthritis who have tried a TNF blocker and have not achieved symptom management.

Pregnancy and Breastfeeding

Xeljanz is not recommended for use during pregnancy or while breastfeeding. The safety and efficacy have not been studied in these patients.

Serious Infections

Patients who take Xeljanz have an increased risk of developing serious infections that may lead to hospitalization or death. Reported infections while taking Xeljanz include pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis. Opportunistic infections have also been reported while taking Xeljanz, including tuberculosis and other mycobacterial infections, cryptococcosis, histoplasmosis, esophageal candidiasis, pneumocystosis, multidermatomal herpes zoster, cytomegalovirus infections, BK virus infection, and listeriosis.

Risks versus benefits should be considered before starting Xeljanz treatment for the following patients

• Patients with chronic or recurrent infections
• Patients who have been exposed to tuberculosis
• Patients with a history of opportunistic infections
• Patients who have traveled to endemic areas
• Patients with underlying conditions that increase the risk of infections such as diabetes

Patients taking Xeljanz require close monitoring for signs of infection. If a severe infection or sepsis develops while taking Xeljanz, it should be discontinued immediately. Patients who develop a new infection while receiving Xeljanz should be closely monitored and treated.

Tuberculosis

Cases of new or reactivated tuberculosis infections have been observed in patients taking Xeljanz. Patients who previously had tested negative for tuberculosis before initiating Xeljanz have developed the disease. Testing for latent TB may be negative while receiving treatment with Xeljanz. Tuberculosis should be strongly considered in patients who develop a new infection while receiving treatment with Xeljanz, especially those that have previously or recently traveled to areas where TB is more prevalent.

Viral Reactivation

Cases of herpes virus and hepatitis B reactivation have been reported with the use of Xeljanz. Patients should be screened for viral hepatitis before starting treatment with Xeljanz.

Cardiovascular Disease

Patients with rheumatoid arthritis aged 50 and older with at least one cardiovascular risk factor who are treated with Xeljanz have a higher overall risk of sudden cardiovascular death. Risk versus benefits should be discussed with patients with any cardiovascular risk factors before starting treatment with Xeljanz.

Cancers

A higher incidence of lymphomas and other forms of cancer has been reported in clinical studies of patients taking Xeljanz. Patients who are current or past smokers carry an additional risk factor of cancer development while taking Xeljanz. Patients should be screened for cancer risk factors before and during treatment with Xeljanz.

Non-melanoma Skin Cancer

Nonmelanoma skin cancers have been reported in patients taking Xeljanz. Periodic skin examinations are recommended while receiving treatment with Xeljanz.

Blood Clots

Blood clots, including pulmonary embolism (PE), deep venous thrombosis (DVT), and arterial thrombosis, have occurred in patients taking Xeljanz. Patients should be instructed to monitor for signs and symptoms of blood clots before initiating treatment. Patients who present with blood clot symptoms should be evaluated promptly, and Xeljanz should be discontinued.

Gastrointestinal Perforations

Gastrointestinal perforations have been reported in patients with rheumatoid arthritis who received treatment with nonsteroidal anti-inflammatory drugs like Xeljanz. Caution should be used in patients with a history of diverticulitis. Patients who present with new onset of abdominal pain should promptly be evaluated for gastrointestinal perforation.

Laboratory Abnormalities.

• Lymphocyte abnormalities have been reported in patients taking Xeljanz. Patients should be monitored periodically for decreased lymphocytes while receiving treatment with Xeljanz. Patients with lymphocytes less than 500 are at an increased risk of serious infections.
• Patients taking Xeljanz have an increased risk of neutropenia (decreased white blood cell counts). Neutrophils should be monitored before starting treatment with Xeljanz, 4-8 weeks after starting treatment, and every three months while receiving treatment.
• Anemia has been reported in patients taking Xeljanz. Patients with low hemoglobin levels should not be started on Xeljanz. Hemoglobin levels should be monitored before initiating treatment with Xeljanz, 4-8 weeks after starting treatment, and every three months after that.
• Elevated liver enzymes have been reported in patients taking Xeljanz. Routine monitoring of liver enzymes is recommended while receiving treatment with Xeljanz. If patients present with drug-induced liver injury symptoms, Xeljanz should be discontinued.
• Lipid elevations have been associated with Xeljanz. Lipids should be assessed intermittently while receiving treatment with Xeljanz.

Live Vaccines

Live vaccinations should not be given concurrently with Xeljanz. It is recommended that pediatric patients receive all live vaccines before starting Xeljanz.

Drug Interactions

This is not a complete list of potential drug interactions. Before taking Xeljanz (Tofacitinib), tell your doctor if you take any medications, herbal supplements, or vitamins.

Strong CP3AF Inhibitors

Ketoconazole, when used with Xeljanz, can increase exposure to the medication. Xeljanz dosage should be decreased if taken with a strong CP3AF Inhibitor.

Moderate CYP3A4 Inhibitors Coadministered with Strong CYP2C19 Inhibitors

Fluconazole used in fungal infections, when given with Xeljanz, can increase the exposure to the medication. Xeljanz dosage should be decreased when used together with these medications.

Strong CYP3A4 Inducers

Rifampin can decrease exposure to Xeljanz and reduce clinical response when given in conjunction with Xeljanz.

Immunosuppressive Drugs

Immunosuppressive drugs such as azathioprine, tacrolimus, and cyclosporine increase the risk of infections when taken with Xeljanz, and coadministration is not recommended.

Alternative Medications

There are other drugs available to treat rheumatoid arthritis and ulcerative colitis. It is important to note that this is not a complete list of alternative treatments; speak to your doctor to discuss other medications.

Hydroxychloroquine (Plaquenil)

Hydroxychloroquine belongs to a class of medications called antimalarials. It works to treat rheumatoid arthritis by decreasing the activity of the immune system.

Sulfasalazine (Azulfidine)

Sulfasalazine belongs to a class of medications called anti-inflammatory drugs. It works to treat rheumatoid arthritis and polyarticular juvenile idiopathic arthritis by reducing inflammation within the body.

Leflunomide (Arava)

Leflunomide belongs to a class of medications called disease-modifying antirheumatic drugs (DMARDs). It treats rheumatoid arthritis by decreasing inflammations and slowing disease progression. Other medicines used to treat rheumatoid arthritis in this class include azathioprine (Imuran).

Tumor Necrosis Factor Inhibitors (TNF)

TNF inhibitors work by blocking TNF production, a protein produced by the body that causes inflammation. Available TNF blockers include etanercept (Enbrel), adalimumab (Humira), and infliximab (Remicade).

Aminosalicylates

Aminosalicylates can be used to treat and maintain mild to moderate ulcerative colitis. These medications work to decrease inflammation in the colon. Other medicines used to treat ulcerative colitis in this class include sulfasalazine (Azulfidine), olsalazine (Dipentum), and balsalazide (Colazal).

Corticosteroids

Corticosteroids can be used to treat moderate to severely active ulcerative colitis. They work by suppressing the immune system, which decreases systemic inflammation. Due to this medication’s short and long-term side effects, it should only be used in active flare-ups and not as maintenance. Other medicines used to treat ulcerative colitis in this class include budesonide (Uceris), hydrocortisone (Cortef), methylprednisolone (Medrol), and prednisone (Rayos).

Immunomodulators

These drugs control and suppress the body’s immune system so that it cannot cause inflammation. These medications can take several months to become effective and are often used with aminosalicylates or corticosteroids. Other medicines used to treat ulcerative colitis in this class include azathioprine (Azasan), 6-mercaptopurine (6-MP), cyclosporine (Sandimmune), and tacrolimus (Protopic).

Biologic Therapies

Biologics are reserved for treating people with moderate to severe ulcerative colitis. They work by providing antibodies that stop the body from causing inflammation. Other medications in this class used to treat ulcerative colitis include adalimumab (Humira), infliximab (Inflectra, Remicade, Renflexis), golimumab (Simponi), and vedolizumab (Entyvio).

Targeted Synthetic Small Molecules

These drugs work to reduce inflammation by targeting the immune system. They are used in patients with moderate to severely active disease. Other medications in this class used to treat ulcerative colitis include ozanimod (Zeposia), tofacitinib (Xeljanz), and upadacitinib (Rinvoq).

Frequently Asked Questions