XELJANZ

What it is

XELJANZ is a medicine containing tofacitinib citrate, available as 5 mg and 10 mg film-coated tablets, XELJANZ XR 11 mg extended release film-coated tablets, and a 1 mg/mL oral solution.

Approved indications —

Moderate to severe active rheumatoid arthritis in adults who have had an inadequate response or are intolerant to methotrexate. — Active psoriatic arthritis in adult patients who have had an inadequate response to a prior DMARD therapy. — Moderately to severely active ulcerative colitis in adult patients who have had an inadequate response, lost response, or were intolerant to either conventional therapy or a biological therapy. — Active ankylosing spondylitis in adult patients who have responded inadequately to conventional therapy. — Active polyarticular course juvenile idiopathic arthritis and juvenile psoriatic arthritis in patients 2 years of age and older who have responded inadequately to previous therapy with DMARDs.

Dosing overview

For juvenile idiopathic arthritis and juvenile psoriatic arthritis in patients 2 years of age and older, the dose is based on body weight: 3.2 mg twice daily for 10 to <20 kg, 4 mg twice daily for 20 to <40 kg, and 5 mg twice daily for ≥40 kg.

Key safety warnings

A large randomised post-marketing safety study in rheumatoid arthritis patients 50 years of age and older with at least one additional cardiovascular risk factor showed a higher rate of all-cause mortality with tofacitinib compared to TNF inhibitors, mainly due to cardiovascular events, infections and malignancies. In this study, patients treated with tofacitinib had a higher rate of major adverse cardiovascular events (MACE), defined as cardiovascular death, non-fatal myocardial infarction and non-fatal stroke compared to TNF inhibitors. MACE was more common in patients 65 years of age and older, current or past long-time smokers, and those with a history of atherosclerotic cardiovascular disease. Serious and sometimes fatal thrombosis events including deep vein thrombosis, arterial thrombosis and pulmonary embolism have occurred in patients treated with tofacitinib, with a dose-dependent increased risk compared to TNF inhibitors in a randomised post-marketing safety study. Lymphomas have been observed in patients treated with XELJANZ, with an increased incidence compared with TNF inhibitors in a large randomised post-marketing safety study in rheumatoid arthritis patients. Lung cancers have been observed in patients treated with XELJANZ, with an increase compared with TNF inhibitor in a large randomised post-marketing safety study. Patients treated with XELJANZ are at increased risk for developing serious infections that may lead to hospitalisation or death, especially in those taking concomitant immunosuppressants. The most common serious infections reported include pneumonia, urinary tract infection, cellulitis, herpes zoster, bronchitis, septic shock, diverticulitis, gastroenteritis, appendicitis and sepsis. Opportunistic infections including tuberculosis, cryptococcus, histoplasmosis, oesophageal candidiasis, pneumocystosis, herpes zoster, cytomegalovirus and listeriosis have been reported. Lymphocyte counts less than 0.75 x 10⁹ cells/L were associated with an increased incidence of serious infections, and it is not recommended to initiate or continue XELJANZ treatment in patients with a confirmed lymphocyte count less than 0.75 x 10⁹ cells/L.

Contraindications

Hypersensitivity to tofacitinib citrate or to any of the excipients. XELJANZ must not be used in combination with biological agents or other potent immunosuppressive agents. XELJANZ should not be used in patients with severe hepatic impairment.

PBS listing

XELJANZ 5 mg tablets are listed on the PBS with 11 items under authority required and streamlined restrictions at an ex-manufacturer price of A$1037.85. XELJANZ 10 mg tablets are listed with 2 PBS items under authority required restriction at an ex-manufacturer price of A$1733.20. XELJANZ oral solution 1 mg per mL (240 mL) is listed with 2 PBS items under authority required and streamlined restrictions at an ex-manufacturer price of A$1037.85.

Regulatory history

XELJANZ 5 mg film-coated tablets were first listed on the ARTG in February 2015. The Pharmaceutical Benefits Scheme recommended XELJANZ in November 2014 for the treatment of severe active rheumatoid arthritis in patients who have failed to respond to or are intolerant of conventional systemic therapies. In November 2017, PBAC recommended XELJANZ for the treatment of active psoriatic arthritis in adult patients who have had an inadequate response or are intolerant to at least one conventional synthetic disease-modifying antirheumatic drug. An AusPAR was approved on 8 November 2018 for psoriatic arthritis in combination with conventional synthetic DMARDs. XELJANZ 10 mg tablets were added to the ARTG in February 2019. PBAC recommended XELJANZ in March 2023 for juvenile idiopathic arthritis and ankylosing spondylitis. XELJANZ XR 11 mg extended release tablets and XELJANZ 1 mg/mL oral solution were registered on the ARTG in January 2023.