(tofacitinib)

Prescribing Information
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2 DOSAGE AND ADMINISTRATION

2 DOSAGE AND ADMINISTRATION

2.1 Recommended Evaluations and Immunization Prior to Treatment Initiation

Prior to initiating XELJANZ (tablets and oral solution) or XELJANZ XR (extended-release tablets), consider performing the following:

•
Active and latent tuberculosis (TB) infection evaluation: If the patient has latent TB, treat for TB prior to XELJANZ/XELJANZ XR treatment [see Warnings and Precautions (5.1)].
•
Viral hepatitis screening in accordance with clinical guidelines [see Warnings and Precautions (5.1)].
•
A complete blood count: Avoid initiation of XELJANZ/XELJANZ XR treatment in patients with a lymphocyte count less than 500 cells/mm3, absolute neutrophil count less than 1000 cells/mm3, or hemoglobin level less than 9 g/dL [see Warnings and Precautions (5.8)].
•
Baseline hepatic function evaluation: XELJANZ/XELJANZ XR is not recommended for patients with severe hepatic impairment [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3)].
•
Update immunizations according to current immunization guidelines. The interval between live vaccinations and initiation of XELJANZ/XELJANZ XR should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions (5.9)].

2.2 Important Administration Instructions

•
XELJANZ XR (extended-release tablets) is not substitutable with XELJANZ (tablets and oral solution). Switching between XELJANZ and XELJANZ XR should be made by the healthcare provider.
•
Dose interruption is recommended for management of lymphopenia, neutropenia, and anemia [see Warnings and Precautions (5.8) and Adverse Reactions (6.1)].
•
Interrupt use of XELJANZ/XELJANZ XR if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1)].
•
Take XELJANZ/XELJANZ XR with or without food [see Clinical Pharmacology (12.3)].
•
Swallow XELJANZ XR whole and intact. Do not crush, split, or chew the extended-release tablets [see Clinical Pharmacology (12.3)].

2.3 Recommended Dosage in Adults with Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

Table 1 displays the recommended dosage of XELJANZ tablets and XELJANZ XR (extended-release tablets) for adults with RA, PsA, and AS [see Indication and Usage (1.1, 1.2, 1.3)] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations (8.6, 8.7)]. The table also displays the recommended dosage modifications for patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3)], and patients with lymphopenia, neutropenia, or anemia.

Table 1: Recommended Dosage of XELJANZ Tablets and XELJANZ XR in Adults with Rheumatoid Arthritis, Psoriatic Arthritis, or Ankylosing Spondylitis
*
Excludes patients who concomitantly use XELJANZ tablets/XELJANZ XR with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
Tofacitinib PK was evaluated in subjects with varying degrees of renal impairment, where the severity of renal impairment was defined based on creatinine clearance (CLcr) estimated using the Cockcroft‑Gault equation: CLcr >80 mL/min (normal renal function); >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); <30 mL/min (severe renal impairment).

Adults

XELJANZ Tablets

XELJANZ XR

(extended-release tablets)

Patients with Normal Renal and Hepatic Function*

5 mg twice daily

11 mg once daily

Recommended Dosage in Patients with Renal Impairment (RI)†

Mild RI

(CLcr >50 and ≤80 mL/min)

5 mg twice daily

11 mg once daily

Moderate RI

(CLcr ≥30 and ≤50 mL/min)

5 mg once daily

XELJANZ tablets 5 mg once daily

Severe RI

(CLcr <30 mL/min)

5 mg once daily

XELJANZ tablets 5 mg once daily

For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.

Recommended Dosage in Patients with Hepatic Impairment (HI)

Mild HI

(Child-Pugh A)

5 mg twice daily

11 mg once daily

Moderate HI

(Child-Pugh B)

5 mg once daily

XELJANZ tablets 5 mg once daily

Severe HI

(Child-Pugh C)

Use of XELJANZ tablets/XELJANZ XR is not recommended.

Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s)

Strong CYP2C19 inhibitor(s)

5 mg twice daily

11 mg once daily

Moderate CYP2C19 inhibitor(s)

Moderate CYP3A4 inhibitor(s)

Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole)

5 mg once daily

XELJANZ tablets 5 mg once daily

Strong CYP3A4 inhibitor(s)

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing. When ANC is greater than 1000, resume 5 mg twice daily.

Interrupt dosing. When ANC is greater than 1000, resume 11 mg once daily.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ tablets 5 mg twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of XELJANZ tablets 5 mg.

2.4 Recommended Dosage in Pediatric Patients 2 Years of Age and Older with Psoriatic Arthritis or Polyarticular Course Juvenile Idiopathic Arthritis

Table 2 displays the recommended body weight-based dosages for XELJANZ tablets and XELJANZ oral solution in pediatric patients 2 years of age and older with PsA or pcJIA [see Indication and Usage (1.2, 1.4)] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations (8.6, 8.7)]. The table also includes recommended dosage modification for pediatric patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3)], and pediatric patients with lymphopenia, neutropenia, or anemia.

Administer XELJANZ oral solution using the included press-in bottle adapter and oral dosing syringe [see Instructions for Use].

Table 2: Recommended Dosage of XELJANZ Tablets and XELJANZ Oral Solution in Pediatric Patients 2 Years of Age and Older with PsA or pcJIA
Pediatric Patients 2 Years of Age and OlderXELJANZ tablets and XELJANZ oral solution
*
Excludes patients who concomitantly use XELJANZ (tablets and oral solution) with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
Patients treated with XELJANZ oral solution 5 mL may be switched to XELJANZ tablets 5 mg.

Patients with Normal Renal and Hepatic Function*

•
10 kg ≤ body weight <20 kg: 3.2 mg (3.2 mL oral solution) twice daily
•
20 kg ≤ body weight <40 kg: 4 mg (4 mL oral solution) twice daily
•
Body weight ≥40 kg: 5 mg (one 5 mg tablet or 5 mL oral solution) twice daily†

Recommended Dosage in Patients with Renal Impairment (RI)

Mild RI

Same as patients with normal renal function.

Moderate RI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Severe RI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.

Recommended Dosage in Patients with Hepatic Impairment (HI)

Mild HI

Same as patients with normal hepatic function.

Moderate HI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Severe HI

Use of XELJANZ tablets/XELJANZ oral solution is not recommended.

Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s)

Strong CYP2C19 inhibitor(s)

No dosage modification is recommended.

Moderate CYP2C19 inhibitor(s)

Moderate CYP3A4 inhibitor(s)

Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole)

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Strong CYP3A4 inhibitor(s)

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing until ANC is greater than 1000 cells/mm3.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

2.5 Recommended Dosage in Adults with Ulcerative Colitis

Table 3 displays the recommended dosage of XELJANZ tablets and XELJANZ XR (extended-release tablets) in adult patients with ulcerative colitis (UC) [see Indications and Usage (1.5)] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations (8.6, 8.7)]. Table 4 displays the recommended dosage modification for patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3)], and patients with lymphopenia, neutropenia, or anemia.

Table 3: Recommended Dosage of XELJANZ Tablets and XELJANZ XR in Adults with Ulcerative Colitis With and Without Renal Impairment or Hepatic Impairment
AdultsXELJANZ
tablets		XELJANZ XR
(extended-release tablets)
*
Excludes patients who concomitantly use XELJANZ tablets/XELJANZ XR with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
Tofacitinib PK was evaluated in subjects with varying degrees of renal impairment, where the severity of renal impairment was defined based on creatinine clearance (CLcr) estimated using the Cockcroft‑Gault equation: CLcr >80 mL/min (normal renal function); CLcr >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); <30 mL/min (severe renal impairment).

Patients with Normal Renal and Hepatic Function*

Induction: 10 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)]; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 10 mg twice daily for a maximum of 16 weeks. Discontinue 10 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.

Induction: 22 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 22 mg once daily for a maximum of 16 weeks. Discontinue 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Maintenance: 5 mg twice daily.

For patients with loss of response during maintenance treatment, may consider a dosage of 10 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient. Use the lowest effective dosage needed to maintain response.

Maintenance: 11 mg once daily.

For patients with loss of response during maintenance treatment, may consider a dosage of 22 mg once daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient. Use the lowest effective dose needed to maintain response.

Recommended Dosage in Patients with Renal Impairment (RI)†

Mild RI
(CLcr >50 and ≤80 mL/min)

Same as patients with normal renal function.

Moderate RI
(CLcr ≥30 and ≤50 mL/min)

Induction: 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)]; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 5 mg twice daily for a maximum of 16 weeks. Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Severe RI
(CLcr <30 mL/min)

Maintenance: 5 mg once daily.
For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient. Use the lowest effective dosage needed to maintain response.


For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.

Maintenance: XELJANZ XR is not recommended. See Maintenance Dosage for XELJANZ tablets for Moderate or Severe RI.


For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.

Recommended Dosage in Patients with Hepatic Impairment (HI)

Mild HI
(Child-Pugh A)

Same as patients with normal hepatic function.

Moderate HI
(Child-Pugh B)

Induction: 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)]; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 5 mg twice daily for a maximum of 16 weeks. Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Maintenance: 5 mg once daily.

For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient. Use the lowest effective dosage needed to maintain response.

Maintenance: XELJANZ XR is not recommended. See Maintenance Dosage for XELJANZ tablets for Moderate HI.

Severe HI
(Child-Pugh C)

Use of XELJANZ tablets/XELJANZ XR is not recommended.

Table 4: Dosage Modifications of XELJANZ Tablets and XELJANZ XR Due to Drug Interactions and for Lymphopenia, Neutropenia or Anemia in Adults with Ulcerative Colitis
AdultsXELJANZ
Tablets		XELJANZ XR
(extended-release tablets)

Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s)

Strong CYP2C19 inhibitor(s)

No dosage modification is recommended.

Moderate CYP2C19 inhibitor(s)

Moderate CYP3A4 inhibitor(s)

Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole)

Induction: 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)]; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 5 mg twice daily for a maximum of 16 weeks. Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Strong CYP3A4 inhibitor(s)

Maintenance: 5 mg once daily.

For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient. Use the lowest effective dosage needed to maintain response.

Maintenance: XELJANZ XR is not recommended. see Maintenance Dosage for XELJANZ tablets for Strong CYP3A4 inhibitors.

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

Lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

ANC less than 500 cells/mm3

Discontinue dosing.

ANC 500 to 1000 cells/mm3

If taking:

•
10 mg twice daily, reduce to 5 mg twice daily. When ANC is greater than 1000, increase to 10 mg twice daily based on clinical response.
•
5 mg twice daily, interrupt dosing. When ANC is greater than 1000, resume 5 mg twice daily.

If taking:

•
22 mg once daily, reduce to 11 mg once daily. When ANC is greater than 1000, increase to 22 mg once daily based on clinical response.
•
11 mg once daily, interrupt dosing. When ANC is greater than 1000, resume 11 mg once daily.

Hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ tablets:

•
5 mg twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of XELJANZ tablets 5 mg.
•
10 mg twice daily may be switched to XELJANZ XR extended-release tablets 22 mg once daily the day following the last dose of XELJANZ tablets 10 mg.
Medication Guide

MEDICATION GUIDE

MEDICATION GUIDE

XELJANZ (ZEL' JANS')
(tofacitinib)
tablets, for oral use

XELJANZ XR (ZEL' JANS' EKS-AHR)
(tofacitinib) extended-release tablets for oral use

XELJANZ (ZEL' JANS')
(tofacitinib)
oral solution

What is the most important information I should know about XELJANZ/XELJANZ XR/XELJANZ oral solution?
XELJANZ/XELJANZ XR/XELJANZ oral solution may cause serious side effects including:

1.

Serious infections. XELJANZ/XELJANZ XR/XELJANZ oral solution are medicines that affect your immune system. XELJANZ/XELJANZ XR/XELJANZ oral solution can lower the ability of your immune system to fight infections. Some people can have serious infections while taking XELJANZ/XELJANZ XR/XELJANZ oral solution, 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 XELJANZ/XELJANZ XR/XELJANZ oral solution and during treatment.
•
Your healthcare provider should monitor you closely for signs and symptoms of TB infection during treatment with XELJANZ/XELJANZ XR/XELJANZ oral solution.

You should not start taking XELJANZ/XELJANZ XR/XELJANZ oral solution if you have any kind of infection unless your healthcare provider tells you it is okay. You may be at a higher risk of developing shingles (herpes zoster).
People with ulcerative colitis taking the higher dose of XELJANZ (10 mg twice daily) or XELJANZ XR (22 mg one time each day) have a higher risk of serious infections and shingles.
Before starting XELJANZ/XELJANZ XR/XELJANZ oral solution, tell your healthcare provider if you:

•
think you have an infection or have symptoms of an infection such as:
 
o
fever, sweating, or chills
o
cough
o
blood in phlegm
o
warm, red, or painful skin or sores on your body
o
burning when you urinate or urinating more often than normal
 
o
muscle aches
o
shortness of breath
o
weight loss
o
diarrhea or stomach pain
o
feeling very tired
•
are being treated for an infection.
•
get a lot of infections or have infections that keep coming back.
•
have diabetes, chronic lung disease, 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 take XELJANZ/XELJANZ XR/XELJANZ oral solution. 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.

After starting XELJANZ/XELJANZ XR/XELJANZ oral solution, call your healthcare provider right away if you have any symptoms of an infection. XELJANZ/XELJANZ XR/XELJANZ oral solution can make you more likely to get infections or make worse any infection that you have.

2.

Increased risk of death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking XELJANZ 5 mg or 10 mg twice daily.

3.

Cancer and immune system problems. XELJANZ/XELJANZ XR/XELJANZ oral solution may increase your risk of certain cancers by changing the way your immune system works.

•
Lymphoma and other cancers including skin cancers can happen in people taking XELJANZ/XELJANZ XR/XELJANZ oral solution. People taking XELJANZ 5 mg twice daily or XELJANZ 10 mg twice daily have a higher risk of certain cancers including lymphoma and lung cancer, especially if you are a current or past smoker. People with ulcerative colitis taking the higher dose of XELJANZ (10 mg twice daily) or XELJANZ XR (22 mg one time each day) have a higher risk of skin cancers. Tell your healthcare provider if you have ever had any type of cancer.

4.

Increased risk of major cardiovascular events such as heart attack, stroke or death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking XELJANZ 5 mg or 10 mg twice daily, especially if you are a current or past smoker.
Get emergency help right away if you have any symptoms of a heart attack or stroke while taking XELJANZ/XELJANZ XR/XELJANZ oral solution, including:

•
discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back
•
severe tightness, pain, pressure, or heaviness in your chest, throat, neck, or jaw
•
pain or discomfort in your arms, back, neck, jaw, or stomach
•
shortness of breath with or without chest discomfort
•
breaking out in a cold sweat
•
nausea or vomiting
•
feeling lightheaded
•
weakness in one part or on one side of your body
•
slurred speech

5.

Blood clots in the lungs, veins of the legs or arms, and arteries. Blood clots in the lungs (pulmonary embolism, PE), veins of the legs (deep vein thrombosis, DVT) and arteries (arterial thrombosis) have happened more often in people who are 50 years of age and older and with at least 1 heart disease (cardiovascular) risk factor taking XELJANZ 5 mg or 10 mg twice daily. Blood clots in the lungs have also happened in people with ulcerative colitis. Some people have died from these blood clots.

•
Stop taking XELJANZ/XELJANZ XR/XELJANZ oral solution and tell your healthcare provider right away if you develop signs and symptoms of a blood clot, such as sudden shortness of breath or difficulty breathing, chest pain, swelling of the leg or arm, leg pain or tenderness, or redness or discoloration in the leg or arm.

6.

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 XELJANZ/XELJANZ XR/XELJANZ oral solution can get tears in their stomach or intestines. 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.

7.

Allergic reactions.

•
Symptoms such as swelling of your lips, tongue, or throat, or hives (raised, red patches of skin that are often very itchy) that may mean you are having an allergic reaction have been seen in people taking XELJANZ/XELJANZ XR. Some of these reactions were serious. If any of these symptoms occur while you are taking XELJANZ/XELJANZ XR/XELJANZ oral solution, stop XELJANZ/XELJANZ XR/XELJANZ oral solution and call your healthcare provider right away.

8.

Changes in certain laboratory test results. Your healthcare provider should do blood tests before you start taking XELJANZ/XELJANZ XR/XELJANZ oral solution and while you take XELJANZ/XELJANZ XR/XELJANZ oral solution 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 take XELJANZ/XELJANZ XR/XELJANZ oral solution 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 XELJANZ/XELJANZ XR/XELJANZ oral solution 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 taking XELJANZ/XELJANZ XR/XELJANZ oral solution, and as needed after that. Normal cholesterol levels are important to good heart health.

See "What are the possible side effects of XELJANZ/XELJANZ XR/XELJANZ oral solution?" for more information about side effects.

What is XELJANZ/XELJANZ XR/XELJANZ oral solution?

•
XELJANZ/XELJANZ XR/XELJANZ oral solution is a prescription medicine called a Janus kinase (JAK) inhibitor. XELJANZ/XELJANZ XR is used to treat adults with moderately to severely active rheumatoid arthritis when 1 or more medicines called tumor necrosis factor (TNF) blockers have been used and did not work well or cannot be tolerated.
•
XELJANZ/XELJANZ XR is used to treat adults and XELJANZ/XELJANZ oral solution is used to treat children 2 years of age and older with active psoriatic arthritis when 1 or more TNF blocker medicines have been used, and did not work well or cannot be tolerated.
•
XELJANZ/XELJANZ XR is used to treat adults with active ankylosing spondylitis when 1 or more TNF blocker medicines have been used and did not work well or cannot be tolerated.
•
XELJANZ/XELJANZ XR is used to treat adults with moderately to severely active ulcerative colitis when 1 or more TNF blocker medicines have been used, and did not work well or cannot be tolerated.
•
XELJANZ/XELJANZ oral solution is used to treat children 2 years of age and older with active polyarticular course juvenile arthritis when 1 or more TNF blocker medicines have been used, and did not work well or cannot be tolerated.

It is not known if XELJANZ/XELJANZ XR/XELJANZ oral solution is safe and effective in people with Hepatitis B or C.
XELJANZ/XELJANZ XR/XELJANZ oral solution is not recommended for people with severe liver problems.
It is not known if XELJANZ/XELJANZ oral solution is safe and effective in children for treatment other than active polyarticular course juvenile arthritis and psoriatic arthritis.
It is not known if XELJANZ XR is safe and effective in children.

What should I tell my healthcare provider before taking XELJANZ/XELJANZ XR/XELJANZ oral solution?
Before taking XELJANZ/XELJANZ XR/XELJANZ oral solution, tell your healthcare provider about all of your medical conditions, including if you:

•
have an infection. See "What is the most important information I should know about XELJANZ/XELJANZ XR/XELJANZ oral solution?"
•
are a current or past smoker.
•
have had any type of cancer.
•
have had a heart attack, other heart problems or stroke.
•
have had blood clots in the veins of your legs, arms, or lungs, or clots in the arteries in the past.
•
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 XELJANZ/XELJANZ XR/XELJANZ oral solution.
•
have recently received or are scheduled to receive a vaccine. People who take XELJANZ/XELJANZ XR/XELJANZ oral solution should not receive live vaccines. People taking XELJANZ/XELJANZ XR/XELJANZ oral solution can receive non-live vaccines.
•
plan to become pregnant or are pregnant. XELJANZ/XELJANZ XR/XELJANZ oral solution may affect the ability of females to get pregnant. It is not known if this will change after stopping XELJANZ/XELJANZ XR/XELJANZ oral solution. It is not known if XELJANZ/XELJANZ XR/XELJANZ oral solution will harm an unborn baby.
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plan to breastfeed or are breastfeeding. You and your healthcare provider should decide if you will take XELJANZ/XELJANZ XR/XELJANZ oral solution or breastfeed. You should not do both. After you stop your treatment with XELJANZ/XELJANZ XR/XELJANZ oral solution do not start breastfeeding again until:
o
18 hours after your last dose of XELJANZ/XELJANZ oral solution or
o
36 hours after your last dose of XELJANZ XR

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. XELJANZ/XELJANZ XR/XELJANZ oral solution and other medicines may affect each other causing side effects.
Especially tell your healthcare provider if you take:

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any other medicines to treat your rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, or polyarticular course juvenile arthritis. You should not take tocilizumab (Actemra), etanercept (Enbrel), adalimumab (Humira), infliximab (Remicade), rituximab (Rituxan), abatacept (Orencia), anakinra (Kineret), certolizumab (Cimzia), golimumab (Simponi), ustekinumab (Stelara), secukinumab (Cosentyx), vedolizumab (Entyvio), ixekizumab (Taltz), azathioprine, cyclosporine, or other immunosuppressive drugs while you are taking XELJANZ/XELJANZ XR/XELJANZ oral solution. Taking XELJANZ/XELJANZ XR/XELJANZ oral solution 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.

How should I take XELJANZ/XELJANZ XR/XELJANZ oral solution?
Take XELJANZ/XELJANZ XR/XELJANZ oral solution exactly as your healthcare provider tells you to take it.

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Take XELJANZ/XELJANZ oral solution 2 times a day with or without food.
•
Take XELJANZ XR 1 time a day with or without food.
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Swallow XELJANZ XR tablets whole and intact. Do not crush, split, or chew.
•
When you take XELJANZ XR, you may see something in your stool that looks like a tablet. This is the empty shell from the tablet after the medicine has been absorbed by your body.
•
If you take too much XELJANZ/XELJANZ XR/XELJANZ oral solution, call your healthcare provider or go to the nearest hospital emergency room right away.
•
For the treatment of psoriatic arthritis, take XELJANZ/XELJANZ XR/XELJANZ oral solution in combination with methotrexate, sulfasalazine or leflunomide as instructed by your healthcare provider.
•
XELJANZ XR should not be used instead of XELJANZ oral solution.

What are the possible side effects of XELJANZ/XELJANZ XR/XELJANZ oral solution?

XELJANZ/XELJANZ XR/XELJANZ oral solution may cause serious side effects, including:

•
See "What is the most important information I should know about XELJANZ/XELJANZ XR/XELJANZ oral solution?"
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Hepatitis B or C activation infection in people who carry the virus in their blood. If you are a carrier of the hepatitis B or C virus (viruses that affect the liver), the virus may become active while you use XELJANZ/XELJANZ XR/XELJANZ oral solution. Your healthcare provider may do blood tests before you start treatment with XELJANZ/XELJANZ XR/XELJANZ oral solution and while you are taking XELJANZ/XELJANZ XR/XELJANZ oral solution. Tell your healthcare provider if you have any of the following symptoms of a possible hepatitis B or C infection:
 
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feel very tired
o
little or no appetite
o
clay-colored bowel movements
o
chills
o
muscle aches
o
skin rash
 
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skin or eyes look yellow
o
vomiting
o
fevers
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stomach discomfort
o
dark urine

Common side effects of XELJANZ/XELJANZ XR/XELJANZ oral solution in people with rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis include:

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upper respiratory tract infections (common cold, sinus infections)
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headache
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diarrhea
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nasal congestion, sore throat, and runny nose (nasopharyngitis)
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high blood pressure (hypertension)
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acne

Common side effects of XELJANZ/XELJANZ XR in people with ulcerative colitis include:

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nasal congestion, sore throat, and runny nose (nasopharyngitis)
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increased cholesterol levels
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headache
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upper respiratory tract infections (common cold, sinus infections)
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increased muscle enzyme levels
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rash
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acne
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diarrhea
•
shingles (herpes zoster)

Common side effects of XELJANZ/XELJANZ oral solution in children with polyarticular course juvenile arthritis and psoriatic arthritis include:

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

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 XELJANZ/XELJANZ XR/XELJANZ oral solution. 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.
You may also report side effects to Pfizer at 1-800-438-1985.

How should I store XELJANZ/XELJANZ XR/XELJANZ oral solution?

•
Store XELJANZ/XELJANZ XR at room temperature between 68°F to 77°F (20°C to 25°C).
•
Store XELJANZ oral solution at room temperature between 68°F to 77°F (20°C to 25°C) in the original bottle and carton to protect from light.
•
Safely throw away XELJANZ oral solution that is out of date or no longer needed. Use XELJANZ oral solution within 60 days of opening the bottle. Throw away (discard) remaining oral solution after 60 days.

Keep XELJANZ/XELJANZ XR/XELJANZ oral solution and all medicines out of the reach of children.

General information about the safe and effective use of XELJANZ/XELJANZ XR/XELJANZ oral solution.
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use XELJANZ/XELJANZ XR/XELJANZ oral solution for a condition for which it was not prescribed. Do not give XELJANZ/XELJANZ XR/XELJANZ oral solution to other people, even if they have the same symptoms you have. It may harm them.
This Medication Guide summarizes the most important information about XELJANZ/XELJANZ XR/XELJANZ oral solution. If you would like more information, talk to your healthcare provider. You can ask your pharmacist or healthcare provider for information about XELJANZ/XELJANZ XR/XELJANZ oral solution that is written for health professionals.

What are the ingredients in XELJANZ 5 mg?
Active ingredient: tofacitinib citrate
Inactive ingredients: croscarmellose sodium, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
What are the ingredients in XELJANZ 10 mg?
Active ingredient: tofacitinib citrate
Inactive ingredients: croscarmellose sodium, FD&C Blue #1/Brilliant Blue FCF Aluminum Lake, FD&C Blue #2/Indigo Carmine Aluminum Lake, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
What are the ingredients in XELJANZ XR 11 mg?
Active ingredient: tofacitinib citrate
Inactive ingredients: cellulose acetate, copovidone, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, and triacetin. Printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron, propylene glycol, and shellac glaze.
What are the ingredients in XELJANZ XR 22 mg?
Active ingredient: tofacitinib citrate
Inactive ingredients: cellulose acetate, copovidone, FD&C Blue #2 Aluminum Lake, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, triacetin, and yellow iron oxide. Printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron oxide, propylene glycol, and shellac glaze.
What are the ingredients in XELJANZ oral solution?
Active ingredient: tofacitinib citrate
Inactive ingredients: grape flavor (natural), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and xylitol.

This Medication Guide may have been updated. For the most recent Medication Guide, please visit www.pfizer.com.

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LAB-0535-16.0

This Medication Guide has been approved by the U.S. Food and Drug Administration.     Revised: October 2025

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