Abstract
Rheumatoid arthritis (RA) is a chronic inflammatory disease primarily affecting the joints and is associated with significant levels of disability and reduced quality of life. Janus kinase (JAK) inhibitors are a relatively new class of small molecule oral treatments and offer an alternative for patients with RA who do not respond to conventional or biologic therapy. Upadacitinib is a JAK inhibitor engineered to be selective for JAK1, and has recently been approved for use in patients with moderate-to-severe RA. The purpose of this article is to provide a comprehensive review of upadacitinib, including preclinical development and characterization, phase I and II studies, and the phase III SELECT program. Ongoing trials of upadacitinib in additional indications, including spondyloarthritis, inflammatory bowel disease, and atopic dermatitis, are also discussed.
Conflict of interest
Yoshiya Tanaka reports speaking fees and/or honoraria from: Daiichi Sankyo Company Ltd, Astellas Pharma Inc., Eli Lilly Japan KK, Chugai Pharmaceutical Co. Ltd, AbbVie GK, Pfizer Japan Inc., YL Biologics, Bristol-Myers Squibb Company, Mitsubishi-Tanabe Pharma Corporation, Novartis, Eisai, Takeda, Teijin, and Janssen Pharmaceutical KK. Research grants from: Asahi-Kasei Pharma Corporation, Mitsubishi-Tanabe Pharma Corporation, Bristol-Myers Squibb Company, Eisai Co. Ltd, Chugai Pharmaceutical Co. Ltd, Takeda Pharmaceutical Company Ltd, Sanofi KK, UCB Japan Co. Ltd, Daiichi Sankyo Company Ltd, Ono Pharmaceutical Co. Ltd.