Rheumatoid Arthritis (RA) is an autoimmune disease characterized by persistent inflammation and
joint damage. The main aim of RA treatment is to control the disease progress. Despite the success of
biologicals like Adalimumab, Atlizumab, infliximab, etc. in treatment of RA, the high cost and associated
immunological adverse effects have triggered discovery of small molecules targeting RA. This review
describes the last 15 years of small molecular drug discovery in RA, focused mainly on preclinical and
Keywords: Janus kinase, peptidyl arginine deiminase, phosphoinositide 3-kinase, rheumatoid arthritis, TNFα-converting
enzyme, Tyrosine kinase.
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