This article reviews data from animal and phase 2 clinical studies assessing the immunomodulatory effects and pharmacokinetics of CP-690,550 (now known as tofacitinib), as well as its efficacy and safety in patients with rheumatoid arthritis (RA). In two rodent models of arthritis, CP-690,550 produced dose-dependent decreases in signs of disease activity compared with untreated controls, reductions in histologically assessed inflammation and articular cartilage damage, and statistically signific...

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This study was one of two 24-week, phase 2b studies undertaken to characterise the efficacy and safety dose-response profile of the oral Janus kinase (JAK) inhibitor tofacitinib. Six doses of tofacitinib (20 mg daily and 1, 3, 5, 10 and 15 mg twice daily) and placebo were compared as add-on therapy in adults with active RA despite methotrexate (MTX) therapy. At week 12, ACR 20 response rates were significantly higher with all tofacitinib doses than with placebo (tofacitinib 45.7–58.1%; 33% place...
This is the first phase 3 study to be published for the oral Janus kinase (JAK) inhibitor tofacitinib. This study investigated tofacitinib as a monotherapy in adults with active rheumatoid arthritis who previously failed to respond to disease modifying anti-rheumatic drugs (DMARDs). The study demonstrated that tofacitinib, compared to placebo, was more likely to be associated with reductions in the signs and symptoms of rheumatoid arthritis and improvement in physical function. 59.8% of patients...