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Tofacitinib

    Brands

    DEA Class; Rx

    Common Brand Names; Xeljanz, Xeljanz XR

    • DMARDs, Immunomodulators; 
    • DMARDs, JAK Inhibitors

    Oral Janus kinase (JAK) inhibitor, a target-specific DMARD
    Used in adults with moderate-to-severe rheumatoid, psoriatic arthritis, or ankylosing spondylitis and pediatric patients with polyarticular juvenile idiopathic arthritis; also used for moderately to severely active ulcerative colitis
    Serious infections and malignancy may occur; increased risk of thrombosis, mortality, heart-related problems, and cancers with use of this drug vs. TNF-inhibitors

    Indicated for moderate-to-severe active rheumatoid arthritis (RA) in adults with an inadequate response or intolerance to ≥1 tumor necrosis factor (TNF) blockers

    Indicated for active psoriatic arthritis in adults who have had an inadequate response or intolerance to ≥1 TNF blockers

    Indicated for adults with moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to ≥1 TNF blockers

    Indicated for active ankylosing spondylitis (AS) in adults who have an inadequate response or are intolerant to ≥1 TNF blockers

    None

    UC

    • Nasopharyngitis (10-14%)

    RA

    • Upper respiratory tract infection (4%)
    • Nasopharyngitis (3-4%)
    • Diarrhea (3-4%)
    • Headache (3-4%)
    • Hypertension (2%)

    UC

    • Elevated cholesterol levels (5-9%)
    • Headache (3-9%)
    • Upper respiratory tract infection (6-7%)
    • Increased blood creatine phosphokinase (3-7%)
    • Rash (3-6%)
    • Diarrhea (2-5%)
    • Herpes zoster (1-5%)
    • Gastroenteritis (3-4%)
    • Anemia (2-4%)
    • Nausea (1-4%)

    Malignancy and lymphoproliferative disorders reported (see Black Box Warnings); malignancies were observed in clinical studies and the postmarketing setting, including, but not limited to, lung cancer, breast cancer, melanoma, prostate cancer, and pancreatic cancer

    GI perforation reported, although role of JAK inhibition in these events is unknown; caution in patients at increased risk for gastrointestinal perforation (eg, diverticulitis)

    Associated with gradual decrease in lymphocyte and neutrophils counts, and hemoglobin levels that may require treatment interruption

    Associated with increased LFTs

    Associated with increase lipid parameters including total cholesterol, LDL, and HDL

    Viral reactivation, including cases of herpes virus reactivation (eg, herpes zoster), reported; hepatitis B reactivation reported; impact on chronic viral hepatitis reactivation unknown; perform screening for viral hepatitis in accordance with clinical guidelines before starting therapy

    Non-melanoma skin cancers (NMSCs) reported; periodic skin examination recommended for patients at increased risk for skin cancer

    Use caution when treating patients with diabetes; higher incidence of infection in diabetic population in general reported

    Diverticulitis reported

    Twice daily dosing of tofacitinib 10 mg or 11 mg tofacitinib XR not recommended in patients with rheumatoid arthritis or psoriatic arthritis

    There is a pregnancy exposure registry that monitors pregnancy outcomes in women during pregnancy

    Adults

    10 mg/day PO for immediate-release tablets or 11 mg/day PO for extended-release tablets for rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis; 20 mg/day PO for immediate-release tablets or 22 mg/day PO for extended-release tablets for ulcerative colitis; investigational doses of 20 mg/day PO for immediate-release tablets have been used for COVID-19.

    Geriatric

    10 mg/day PO for immediate-release tablets or 11 mg/day PO for extended-release tablets for rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis; 20 mg/day PO for immediate-release tablets or 22 mg/day PO for extended-release tablets for ulcerative colitis; investigational doses of 20 mg/day PO for immediate-release tablets have been used for COVID-19.

    Adolescents

    Weighing 40 kg or more: 10 mg/day PO immediate-release formulations.
    Weighing 20 to 39 kg: 8 mg/day PO immediate-release formulations.

    Children

    2 to 12 years weighing 40 kg or more: 10 mg/day PO immediate-release formulations.
    2 to 12 years weighing 20 to 39 kg: 8 mg/day PO immediate-release formulations.
    2 to 12 years weighing 10 to 19 kg: 6.4 mg/day PO immediate-release formulations.
    1 year: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    tofacitinib

    tablet (Xeljanz)

    • 5mg
    • 10mg

    tablet, extended-release (Xeljanz XR)

    • 11mg
    • 22mg