Generic Name and Formulations:
Tofacitinib 5mg; tabs.
|Updated Warnings/Precautions re: monitoring lymphocytes, neutrophils, hemoglobin.|
Moderately-to-severely active rheumatoid arthritis (RA) in adults 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).
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. Concomitant potent CYP3A4 inducers: not recommended. 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, active TB (even if initial latent test is negative), or reactivation of herpes virus occurs; interrupt treatment if serious or opportunistic infection, or sepsis develops. Known malignancy. History of GI perforations. 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. Elderly. Pregnancy (Cat.C). 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.
Upper respiratory tract infections, headache, diarrhea, nasopharyngitis; serious or opportunistic infections, TB, malignancies (eg, lymphoma), non-melanoma skin cancer.
Hepatic (CYP3A4, 2C19).
Tabs—28, 60, 180