Treatment of adults with moderately-to-severely active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to methotrexate (MTX); may be used as monotherapy or in combination with MTX or other nonbiologic disease-modifying anti-rheumatic drugs (DMARDs). Do not use in combination with biologic DMARDs or potent immunosuppressants (eg, azathioprine, cyclosporine).
5mg twice daily. Moderate-to-severe renal impairment or moderate hepatic impairment; concomitant potent CYP3A4 inhibitors, or drugs that result in both moderate CYP3A4 and potent CYP2C19 inhibition: 5mg once daily. Dose adjustments: see full labeling.
Janus kinase (JAK) inhibitor.
Increased risk of serious or fatal infections (eg, TB, bacterial, viral, invasive fungal, or other opportunistic pathogens). Active infections: do not initiate therapy. Chronic or history of recurring infections. Travel to, or residence in, areas with endemic TB or mycoses. Conditions that predispose to infection. Test/treat latent TB infection prior to initiating therapy. Monitor closely if new infection, or active TB (even if initial latent test is negative) occurs; interrupt treatment if serious or opportunistic infection, or sepsis develops. Known malignancy. History of GI perforations. Monitor lymphocytes, neutrophils, hemoglobin at baseline and during treatment; do not initiate therapy if lymphocytes <500cells/mm3, ANC <1000cells/mm3, or hemoglobin <9g/dL. Severe hepatic impairment: not recommended. Routinely monitor liver enzymes; interrupt therapy if drug-induced liver injury suspected. Monitor lipids 4–8 weeks following initiation. Elderly. Pregnancy (Cat. C). Nursing mothers: not recommended.
Concomitant live vaccines: not recommended. Potentiated by potent CYP3A4 inhibitors (eg, ketoconazole), or drugs that result in both moderate CYP3A4 and potent CYP2C19 (eg, fluconazole) inhibition. Antagonized by potent CYP3A4 inducers (eg, rifampin). Concomitant immunosuppressants (eg, azathioprine, tacrolimus, cyclosporine) or corticosteroids may increase risk of infections.
Upper respiratory tract infections, headache, diarrhea, nasopharyngitis; serious or opportunistic infections, TB, malignancies (eg, lymphoma).
Hepatic (CYP3A4, 2C19).
Tabs—28, 60, 180