REVIEW Tofacitinib (CP-690,550; CP-690550; CP690550), an orally active immunosuppressant, is being developed by Pfizer for the treatment of rheumatoid arthritis, inflammatory bowel disease, dry eyes, ankylosing spondylitis, psoriasis, psoriatic arthritis, and for the prevention of transplant rejection. Tofacitinib specifically inhibits Janus activated kinase 3 (JAK3), which has a pivotal role in cytokine signal transduction that governs lymphocyte survival, proliferation, differentiation, and apoptosis. It is currently approved for the treatment of rheumatoid arthritis (RA) in the United States and is being studied for treatment of psoriasis, inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. Tofacitinib was not approved by the European regulatory agencies because of concerns over efficacy and safety.
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Mark E. Flanagan, Todd A. Blumenkopf, William H. Brissette, Matthew F. Brown, Jeffrey M. Casavant, Chang Shang-Poa, Jonathan L. Doty, Eileen A. Elliott, Michael B. Fisher, Michael Hines, Craig Kent, Elizabeth M. Kudlacz, Brett M. Lillie, Kelly S. Magnuson, Sandra P. McCurdy, Michael J. Munchhof, Bret D. Perry, Perry S. Sawyer, Timothy J. Strelevitz, Chakrapani Subramanyam, Jianmin Sun, David A. Whipple, and Paul S. Changelian, Disocovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection, Journal of Medicinal Chemistry (2010), 53(24), 8468-8484.
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Kremer JM, Bloom BJ, Breedveld FC, Coombs JH, Fletcher MP, Gruben D, Krishnaswami S, Burgos-Vargas R, Wilkinson B, Zerbini CA, Zwillich SH. The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo. Arthritis Rheum. 2009 Jul;60(7):1895-905. doi: 10.1002/art.24567.
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