Tofacitinib: A Review of its Use in Adult Patients with Rheumatoid Arthritis

Tofacitinib (Xeljanz(A (R))) is the first approved drug in a new class of disease modifying antirheumatic drugs (DMARDs), the Janus kinase (JAK) inhibitors. JAKs have a pivotal role in triggering cytokine-induced signal transduction pathways that influence normal and pathological cellular processes of haematopoiesis and immune cell function, including pathogenic mechanisms involved in rheumatoid arthritis (RA). Selective inhibition of JAKs by tofacitinib potentially modulates inflammatory processes and provides a novel approach for the treatment of RA. Oral tofacitinib is indicated for the treatment of adult patients with active RA who have had an inadequate response to methotrexate and/or other DMARDs. In several large well designed trials, tofacitinib, in combination with methotrexate or other nonbiological DMARDs or as monotherapy, was an effective and generally well tolerated DMARD for the treatment of adult patients with moderately to severely active RA who had had an inadequate response to previous DMARDs, including tumour necrosis factor-alpha inhibitors. Direct head-to-head trials and/or further clinical experience (including long-term safety data), along with robust pharmacoeconomic studies, are required to more definitively position tofacitinib relative to other currently available DMARDs. In the meantime, tofacitinib (alone or in combination with nonbiological DMARDs) is an emerging option for the treatment of DMARD-experienced adult patients with moderately to severely active RA who have had an inadequate response to or are intolerant of methotrexate or other DMARDs.