XELJANZ / XELJANZ XR Highlights

(tofacitinib)

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use XELJANZ/XELJANZ XR/XELJANZ Oral Solution safely and effectively. See full prescribing information for XELJANZ/XELJANZ XR/XELJANZ Oral Solution.

XELJANZ (tofacitinib) tablets, for oral use
XELJANZ XR (tofacitinib) extended-release tablets, for oral use
XELJANZ (tofacitinib) Oral Solution
Initial U.S. Approval: 2012

WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), AND THROMBOSIS

See full prescribing information for complete boxed warning.

  • Increased risk of serious bacterial, fungal, viral, and opportunistic infections leading to hospitalization or death, including tuberculosis (TB). Interrupt treatment with XELJANZ/XELJANZ XR/XELJANZ Oral Solution if serious infection occurs until the infection is controlled. Test for latent TB before and during therapy; treat latent TB prior to use. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test. (5.1)
  • Higher rate of all-cause mortality, including sudden cardiovascular death with XELJANZ vs. TNF blockers in rheumatoid arthritis (RA) patients. (5.2)
  • Malignancies have occurred in patients treated with XELJANZ. Higher rate of lymphomas and lung cancers with XELJANZ vs. TNF blockers in RA patients. (5.3)
  • Higher rate of MACE (defined as cardiovascular death, myocardial infarction, and stroke) with XELJANZ vs. TNF blockers in RA patients. (5.4)
  • Thrombosis has occurred in patients treated with XELJANZ. Increased incidence of pulmonary embolism, venous and arterial thrombosis with XELJANZ vs. TNF blockers in RA patients. (5.5)

RECENT MAJOR CHANGES

Boxed Warning12/2021
Indications and Usage (1)12/2021
Dosage and Administration (2.2)12/2021
Warnings and Precautions (5.2)12/2021
Warnings and Precautions (5.3)12/2021
Warnings and Precautions (5.4)12/2021
Warnings and Precautions (5.5)12/2021

INDICATIONS AND USAGE

XELJANZ/XELJANZ XR/XELJANZ Oral Solution is a Janus kinase (JAK) inhibitor indicated for:

  • Rheumatoid Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.1)
  • Psoriatic Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.2)
  • Ankylosing Spondylitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.3)
  • Ulcerative Colitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biological therapies for UC or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.4)
  • Polyarticular Course Juvenile Idiopathic Arthritis: XELJANZ/XELJANZ Oral Solution is indicated for the treatment of active polyarticular course juvenile idiopathic arthritis (pcJIA) in patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ Oral Solution in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.5)

DOSAGE AND ADMINISTRATION

Administration Instructions

  • XELJANZ XR (tofacitinib extended-release tablets) is not interchangeable or substitutable with XELJANZ Oral Solution. (2.1)
  • Changes between XELJANZ and XELJANZ XR should be made by the healthcare provider. (2.1)
  • Do not initiate XELJANZ/XELJANZ XR/XELJANZ Oral Solution if absolute lymphocyte count <500 cells/mm3, an absolute neutrophil count (ANC) <1000 cells/mm3 or hemoglobin <9 g/dL. (2.1)

Recommended Dosage

Rheumatoid Arthritis

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Psoriatic Arthritis (in combination with nonbiologic DMARDs)

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Ankylosing Spondylitis

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Ulcerative Colitis

  • Induction: XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily for 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed, continue XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily for a maximum of 16 weeks. Discontinue XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved. (2.3)
  • Maintenance: XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. For patients with loss of response during maintenance treatment, XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily may be considered and 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. (2.3)
  • Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment: see full prescribing information. (2.3)

Polyarticular Course Juvenile Idiopathic Arthritis

  • XELJANZ/XELJANZ Oral Solution 5 mg twice daily or weight-based equivalent twice daily. (2.4)
  • Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment: see full prescribing information. (2.4)

Dosage Adjustment

  • See the full prescribing information for dosage adjustments by indication for patients receiving CYP2C19 and/or CYP3A4 inhibitors; in patients with moderate or severe renal impairment or moderate hepatic impairment; and patients with lymphopenia, neutropenia, or anemia. (2.2, 2.3, 2.4, 8.7, 8.8)
  • Use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution in patients with severe hepatic impairment is not recommended in any patient population. (2.2, 2.3, 2.4, 8.8)

DOSAGE FORMS AND STRENGTHS

  • XELJANZ Tablets: 5 mg, 10 mg tofacitinib (3)
  • XELJANZ XR Tablets: 11 mg, 22 mg tofacitinib (3)
  • XELJANZ Oral Solution: 1 mg/mL tofacitinib (3)

CONTRAINDICATIONS

None (4)

WARNINGS AND PRECAUTIONS

  • Serious Infections: Avoid use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution during an active serious infection, including localized infections. (5.1)
  • Gastrointestinal Perforations: Use with caution in patients that may be at increased risk. (5.6)
  • Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. (5.8)
  • Immunizations: Live vaccines: Avoid use with XELJANZ/XELJANZ XR/XELJANZ Oral Solution. (5.9)

ADVERSE REACTIONS

Most common adverse reactions are:

  • Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis: Reported during the first 3 months in rheumatoid arthritis placebo-controlled clinical trials and occurring in ≥2% of patients treated with XELJANZ monotherapy or in combination with DMARDs: upper respiratory tract infection, nasopharyngitis, diarrhea, and headache. (6.1)
  • Ulcerative Colitis: Reported in ≥5% of patients treated with either 5 mg or 10 mg twice daily of XELJANZ and ≥1% greater than reported in patients receiving placebo in either the induction or maintenance clinical trials: nasopharyngitis, elevated cholesterol levels, headache, upper respiratory tract infection, increased blood creatine phosphokinase, rash, diarrhea, and herpes zoster. (6.1)
  • Polyarticular Course Juvenile Idiopathic Arthritis: Consistent with common adverse reactions reported in adult rheumatoid arthritis patients. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer, Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

See full prescribing information for clinically relevant drug interactions. (2, 7)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and Medication Guide.

Revised: 1/2022

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Highlights

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use XELJANZ/XELJANZ XR/XELJANZ Oral Solution safely and effectively. See full prescribing information for XELJANZ/XELJANZ XR/XELJANZ Oral Solution.

XELJANZ (tofacitinib) tablets, for oral use
XELJANZ XR (tofacitinib) extended-release tablets, for oral use
XELJANZ (tofacitinib) Oral Solution
Initial U.S. Approval: 2012

WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), AND THROMBOSIS

See full prescribing information for complete boxed warning.

  • Increased risk of serious bacterial, fungal, viral, and opportunistic infections leading to hospitalization or death, including tuberculosis (TB). Interrupt treatment with XELJANZ/XELJANZ XR/XELJANZ Oral Solution if serious infection occurs until the infection is controlled. Test for latent TB before and during therapy; treat latent TB prior to use. Monitor all patients for active TB during treatment, even patients with initial negative latent TB test. (5.1)
  • Higher rate of all-cause mortality, including sudden cardiovascular death with XELJANZ vs. TNF blockers in rheumatoid arthritis (RA) patients. (5.2)
  • Malignancies have occurred in patients treated with XELJANZ. Higher rate of lymphomas and lung cancers with XELJANZ vs. TNF blockers in RA patients. (5.3)
  • Higher rate of MACE (defined as cardiovascular death, myocardial infarction, and stroke) with XELJANZ vs. TNF blockers in RA patients. (5.4)
  • Thrombosis has occurred in patients treated with XELJANZ. Increased incidence of pulmonary embolism, venous and arterial thrombosis with XELJANZ vs. TNF blockers in RA patients. (5.5)

RECENT MAJOR CHANGES

Boxed Warning12/2021
Indications and Usage (1)12/2021
Dosage and Administration (2.2)12/2021
Warnings and Precautions (5.2)12/2021
Warnings and Precautions (5.3)12/2021
Warnings and Precautions (5.4)12/2021
Warnings and Precautions (5.5)12/2021

INDICATIONS AND USAGE

XELJANZ/XELJANZ XR/XELJANZ Oral Solution is a Janus kinase (JAK) inhibitor indicated for:

  • Rheumatoid Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.1)
  • Psoriatic Arthritis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.2)
  • Ankylosing Spondylitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.3)
  • Ulcerative Colitis: XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biological therapies for UC or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.4)
  • Polyarticular Course Juvenile Idiopathic Arthritis: XELJANZ/XELJANZ Oral Solution is indicated for the treatment of active polyarticular course juvenile idiopathic arthritis (pcJIA) in patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers.
    • Limitations of Use: Use of XELJANZ/XELJANZ Oral Solution in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. (1.5)

DOSAGE AND ADMINISTRATION

Administration Instructions

  • XELJANZ XR (tofacitinib extended-release tablets) is not interchangeable or substitutable with XELJANZ Oral Solution. (2.1)
  • Changes between XELJANZ and XELJANZ XR should be made by the healthcare provider. (2.1)
  • Do not initiate XELJANZ/XELJANZ XR/XELJANZ Oral Solution if absolute lymphocyte count <500 cells/mm3, an absolute neutrophil count (ANC) <1000 cells/mm3 or hemoglobin <9 g/dL. (2.1)

Recommended Dosage

Rheumatoid Arthritis

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Psoriatic Arthritis (in combination with nonbiologic DMARDs)

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Ankylosing Spondylitis

  • XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. (2.2)
  • Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is XELJANZ 5 mg once daily. (2, 8.7, 8.8)

Ulcerative Colitis

  • Induction: XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily for 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed, continue XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily for a maximum of 16 weeks. Discontinue XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved. (2.3)
  • Maintenance: XELJANZ 5 mg twice daily or XELJANZ XR 11 mg once daily. For patients with loss of response during maintenance treatment, XELJANZ 10 mg twice daily or XELJANZ XR 22 mg once daily may be considered and 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. (2.3)
  • Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment: see full prescribing information. (2.3)

Polyarticular Course Juvenile Idiopathic Arthritis

  • XELJANZ/XELJANZ Oral Solution 5 mg twice daily or weight-based equivalent twice daily. (2.4)
  • Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment: see full prescribing information. (2.4)

Dosage Adjustment

  • See the full prescribing information for dosage adjustments by indication for patients receiving CYP2C19 and/or CYP3A4 inhibitors; in patients with moderate or severe renal impairment or moderate hepatic impairment; and patients with lymphopenia, neutropenia, or anemia. (2.2, 2.3, 2.4, 8.7, 8.8)
  • Use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution in patients with severe hepatic impairment is not recommended in any patient population. (2.2, 2.3, 2.4, 8.8)

DOSAGE FORMS AND STRENGTHS

  • XELJANZ Tablets: 5 mg, 10 mg tofacitinib (3)
  • XELJANZ XR Tablets: 11 mg, 22 mg tofacitinib (3)
  • XELJANZ Oral Solution: 1 mg/mL tofacitinib (3)

CONTRAINDICATIONS

None (4)

WARNINGS AND PRECAUTIONS

  • Serious Infections: Avoid use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution during an active serious infection, including localized infections. (5.1)
  • Gastrointestinal Perforations: Use with caution in patients that may be at increased risk. (5.6)
  • Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. (5.8)
  • Immunizations: Live vaccines: Avoid use with XELJANZ/XELJANZ XR/XELJANZ Oral Solution. (5.9)

ADVERSE REACTIONS

Most common adverse reactions are:

  • Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis: Reported during the first 3 months in rheumatoid arthritis placebo-controlled clinical trials and occurring in ≥2% of patients treated with XELJANZ monotherapy or in combination with DMARDs: upper respiratory tract infection, nasopharyngitis, diarrhea, and headache. (6.1)
  • Ulcerative Colitis: Reported in ≥5% of patients treated with either 5 mg or 10 mg twice daily of XELJANZ and ≥1% greater than reported in patients receiving placebo in either the induction or maintenance clinical trials: nasopharyngitis, elevated cholesterol levels, headache, upper respiratory tract infection, increased blood creatine phosphokinase, rash, diarrhea, and herpes zoster. (6.1)
  • Polyarticular Course Juvenile Idiopathic Arthritis: Consistent with common adverse reactions reported in adult rheumatoid arthritis patients. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer, Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

See full prescribing information for clinically relevant drug interactions. (2, 7)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and Medication Guide.

Revised: 1/2022
Medication Guide

Health Professional Information

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