Xeljanz/Xeljanz XR

Tofacitinib citrate

Moderate to severe active RA in adults who had inadequate response to ≥1 DMARDs.

Xeljanz RA 5 mg bid, as monotherapy or in combination w/ MTX or other nonbiologic DMARDs. Patient w/ severe renal impairment, moderate hepatic impairment, & receiving CYP3A4 & CYP2C19 inhibitors Max: 5 mg bid. Xeljanz XR RA 11 mg once daily, as monotherapy or in combination w/ MTX or other nonbiologic DMARDs. Patient w/ severe renal impairment, moderate hepatic impairment & receiving CYP3A4 & CYP2C19 inhibitors Should not exceed 5 mg bid (Xeljanz) or should not exceed 11 mg once daily (Xeljanz XR)

May be taken with or without food: Xeljanz XR Swallow whole, do not crush/split/chew.

Hypersensitivity (eg, angioedema & urticaria). Do not initiate in patients w/ active infection including localized infections; interrupt treatment if serious/opportunistic infection or sepsis develops. Diabetic patients. History of chronic lung disease. Higher infection risk in patients w/ increasing degrees of lymphopenia. Evaluate & test patients for latent or active infection prior to & during administration; consider anti-TB therapy in patients w/ past history of latent or active TB in whom an adequate course of therapy cannot be confirmed, & for patient w/ -ve test for latent TB but who have risk factors for TB infection (closely monitor for development of signs & symptoms prior to initiating therapy). Perform viral hepatitis screening before starting therapy. Higher risk of herpes zoster in Japanese & Korean patients. Assess patients for VTE risk factors before starting & periodically during treatment. Current or past smokers; patients w/ other CV risk factors. Current or history of malignancy other than a successfully treated non-melanoma skin cancer or development of malignancy. Higher risk of lymphoma in patients w/ RA, particularly those w/ highly active disease. Periodic skin exam for patients at increased risk for skin cancer. Patients at increased risk for GI perforation (eg, history of diverticulitis). Evaluate promptly for early identification of GI perforation in patients presenting w/ new onset abdominal symptoms. Not recommended to initiate in patients w/ low lymphocyte count (ie, <500 cells/mm³), low neutrophil count (ie, ANC <1,000 cells/mm³), or low Hb values (ie, <9 g/dL). Monitor lymphocyte at baseline every 3 mth thereafter; neutrophil & Hb at baseline & after 4-8 wk of treatment every 3 mth thereafter. Perform assessment of lipid parameters approx 4-8 wk following initiation of therapy. Do not give concurrently w/ live vaccines; vaccination should occur at least 2 wk but preferably 4 wk before initiating therapy. Avoid in RA patients treated in combination w/ biological DMARDs eg, TNF antagonist, IL-1R antagonist, IL-6R antagonist, anti-CD20 monoclonal Ab(s) & selective co-stimulation modulators & potent immunosuppressants eg, azathioprine & cyclosporine. Not to be used in patients w/ severe hepatic impairment. Effective contraception during treatment & for at least 4 wk after the last dose in women of reproductive potential. Pregnancy. Should not be used during lactation. Neonates & childn <18 yr. Elderly. Xeljanz XR Pre-existing severe GI narrowing (pathologic or iatrogenic).

Pneumonia, flu, herpes zoster, UTI, sinusitis, bronchitis, nasopharyngitis, pharyngitis; anemia; hyperlipidemia; headache; HTN; cough; abdominal pain, vomiting, diarrhea, nausea, gastritis, dyspepsia; rash; arthralgia; pyrexia, peripheral edema, fatigue; increased γ-glutamyltransferase, blood cholesterol, wt & blood creatinine phosphokinase.

Increased exposure w/ potent CYP3A4 inhibitors (eg, ketoconazole), moderate CYP3A4 & potent CYP2C19 inhibitors (eg, fluconazole). Decreased exposure w/ potent CYP inducers (eg, rifampin). Increased AUC & decreased C_max w/ tacrolimus & cyclosporine.

Disease-Modifying Anti-Rheumatic Drugs (DMARDs) / Immunosuppressants

L04AF01 - tofacitinib ; Belongs to the class of Janus-associated kinase (JAK) inhibitors. Used as immunosuppressants.

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