Abstract
Upadacitinib is a selective and reversible Janus kinase (JAK) inhibitor recently approved by the European Medicine Agency and the Food and Drug Administration for the treatment of rheumatoid arthritis (RA) at a dose of 15 mg/day. We present the chemical structure and mechanism of action of upadacitinib together with a comprehensive review of the efficacy of this drug in RA based on the SELECT clinical trial program and its safety profile. Its role in the management and therapeutic strategy of RA is also discussed. Upadacitinib in the different clinical trials has shown similar rates of clinical response, including the remission rates, regardless of the population analyzed (methotrexate-naïve, methotrexate-failure or biologic failure). In a head-to-head randomized clinical trial, upadacitinib plus methotrexate was superior to adalimumab when given on background methotrexate (MTX) in patients who have experienced an inadequate response to MTX. Upadacitinib also demonstrated superiority over abatacept in patients with RA after failure to previous biologic drugs. The safety profile of upadacitinib is generally consistent with those observed with biological or other JAK inhibitors.