Always refer to full SmPC before prescribing XELJANZ.

Tablets shown in the above image are not true to size.

• XELJANZ 5 mg film-coated or 11mg prolonged release tablets can be given with or without food.
• For patients who have difficulties swallowing, XELJANZ 5 mg tablets may be crushed and taken with water. Whereas, XELJANZ 11 mg tablet must be taken whole in order to ensure the entire dose is delivered correctly. They must not be crushed, split or chewed.
• No dose adjustment is required when used in combination with MTX.
• XELJANZ treatment should be interrupted if a patient develops a serious infection until the infection is controlled.
• Rapid absorption in healthy human subjects with plasma concentrations peaking approximately 1 hour after administration of 5 mg tablets. Following oral administration of tofacitinib 11 mg tablet, peak plasma concentrations are reached at 4 hours.
• Terminal half-life of approximately 3 hours for XELJANZ 5 mg tablets and approximately 6 hours for XELJANZ 11 mg tablet.
• XELJANZ 5 mg tablets is available in a 28-day treatment pack.
• XELJANZ 11 mg tablets is available in HDPE (High Density Polyethylene) bottles with 2 silica gel desiccants and child-resistant, polypropylene closure containing 30 or 90 prolonged-release tablets. Or availble as aluminium foil/PVC backed aluminium foil blisters containing 7 prolonged-release tablets. Each pack contains 28 or 91 prolonged-release tablets.

• Hypersensitivity to the active substance of XELJANZ or to any of its excipients*
• Active tuberculosis (TB), serious infections such as sepsis, or opportunistic infections
• Severe hepatic impairment
• Pregnancy and lactation

XELJANZ should only be used if no suitable treatment alternatives are available in patients:

• 65 years of age and older;
• patients with history of atherosclerotic cardiovascular disease or other cardiovascular risk factors (e.g. current or past long-term smokers);
• patients with malignancy risk factors (e.g. current malignancy or history of malignancy (other than a successfully treated non-melanoma skin cancer))

• XELJANZ dose should be reduced to 5 mg once-daily in patients with severe renal impairment (creatinine clearance <30 mL/min).
• For severe renal impairment (including patients undergoing haemodialysis) (creatinine clearance < 30 mL/min), XELJANZ dose should be reduced to 5 mg film-coated tablet once daily when the indicated dose in the presence of normal renal function is 11 mg prolonged-release tablet once daily
• Patients with severe renal impairment should remain on a reduced dose of 5 mg once-daily even after haemodialysis.

• XELJANZ dose should be reduced to 5 mg once daily in patients with moderate hepatic impairment (Child Pugh B).
• XELJANZ should not be used in patients with severe hepatic impairment (Child Pugh C).
• For moderate hepatic impairment, XELJANZ dose should be reduced to 5 mg film-coated tablets once daily when the indicated dose in the presence of normal hepatic function is 11 mg prolonged-release tablet once daily

• No dose adjustment is required in patients 65 years of age and older based on age alone (see other special populations). There are limited data in patients aged 75 years and older.
• Considering the increased risk of serious infections in patients 65 years of age and older, XELJANZ should only be used in these patients if no suitable treatment alternatives are available.

• XELJANZ dose should be reduced to 5 mg once daily in patients receiving potent inhibitors of CYP3A4 (e.g., ketoconazole).^†
• XELJANZ dose should also be reduced to 5 mg once daily in patients receiving one or more concomitant medicines that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g., fluconazole).^†
• Co-administration of XELJANZ with potent CYP inducers (e.g., rifampicin) may result in a loss of, or reduced, clinical response.
• Co-administration of potent inducers of CYP3A4 with XELJANZ is not recommended.

^†XELJANZ dose should be reduced to 5 mg once daily in patients receiving 11 mg once daily.

Note, the licensed dose of XELJANZ for the treatment of PsA in the UK is 5mg administered twice daily or one 11 mg prolonged-release tablet administered once daily, which should not be exceeded.

AUC - area under curve; C_max - maximum concentration; MTX - methotrexate; TB - tuberculosis; RA - rheumatoid arthritis; PsA - psoriatic arthritis; OD - once daily

References