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Drugs Fut 2009, 34(8): 618
ISSN 0377-8282
e-ISSN 2013-0368
Copyright 2009 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2009.034.08.1401067
McCall, M., Merani, S., Toso, C., Shapiro, A.M.J.
Sotrastaurin (AEB-071, NVP-AEB-071) is an orally bioavailable compound that exerts its effects through the selective inhibition of the classic and novel forms of protein kinase C (PKC), thereby inhibiting early T-cell activation and IL-2 production. In preclinical studies, sotrastaurin reduced the rejection of allogeneic solid organ and islet transplants and interacted in a synergistic manner with the immunosuppressive agent ciclosporin. Sotrastaurin is being investigated in a number of clinical trials aimed at exploring its efficacy and safety in T-cell-mediated conditions such as transplant rejection, psoriasis, uveitis and ulcerative colitis. The compound has shown acceptable toxicity profiles in healthy individuals and transplant recipients. Provided sotrastaurin shows continued promise in the ongoing clinical studies, it may be a safe and effective alternative or adjunct to calcineurin inhibitors.

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