Generic Name and Formulations:
Tofacitinib 5mg; tabs.
Indications for XELJANZ:
Moderately-to-severely active rheumatoid arthritis (RA) in adults who have had an inadequate response or intolerance to methotrexate (MTX), as monotherapy or in combination with MTX or other nonbiologic disease-modifying anti-rheumatic drugs (DMARDs). Active psoriatic arthritis in adults who have had an inadequate response or intolerance to MTX or other DMARDs, in combination with nonbiologic DMARDs.
5mg twice daily. Switching from immediate-rel to XR tabs: start XR tabs the day following the last immediate-rel 5mg dose. 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. Concomitant potent CYP3A4 inducers: not recommended. Dose adjustments: see full labeling.
Increased risk of serious or fatal infections (eg, TB, bacterial, viral, invasive fungal, or other opportunistic pathogens). Avoid in active, serious, or localized infections. Chronic, recurrent, or history of serious or opportunistic infections. Travel to, or residence in, areas with endemic TB or mycoses. Conditions that predispose to infection. Test/treat latent TB infection prior to and per applicable guidelines during therapy. Monitor closely if new infection, active TB (even if initial latent test is negative), reactivation of herpes virus or hepatitis occurs; interrupt treatment if serious or opportunistic infection, or sepsis develops. History of chronic lung disease or in those who develop interstitial lung disease. Known malignancy. History of GI perforations. Specifically XR tabs: pre-existing severe GI narrowing. Lymphopenia. Monitor lymphocytes at baseline, then every 3 months; neutrophils and hemoglobin at baseline, after 4–8 weeks, then every 3 months thereafter. 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. Perform periodic skin exam in those with skin cancer risk. Update immunization based on current guidelines prior to initiating therapy. Diabetes. Elderly. Pregnancy. Females of reproductive potential should use effective contraception during and for ≥4wks after last dose. Nursing mothers: not recommended.
Concomitant live vaccines, biologic DMARDs or potent immunosuppressants (eg, azathioprine, cyclosporine): 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); see Adults.
Janus kinase (JAK) inhibitor.
Upper respiratory tract infections, headache, diarrhea, nasopharyngitis; serious or opportunistic infections, TB, malignancies (eg, lymphoma), cytopenias, liver enzyme or lipid elevations, non-melanoma skin cancer.
Hepatic (CYP3A4, 2C19).
Tabs—28, 60, 180; XR tabs—14, 30