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SAR and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine to Prevent Graft Rejection and Treat Psoriasis

Wagner, Juergen and Von Matt, Peter and Faller, Bernard and Cooke, Nigel Graham and Albert, Rainer and Sedrani, Richard and Beerli, Christian and Weckbecker, Gisbert and Evenou, Jean-Pierre and Zenke, Gerhard and Cottens, Sylvain (2011) SAR and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine to Prevent Graft Rejection and Treat Psoriasis. Journal of Medicinal Chemistry, 54 (17). pp. 6028-6039. ISSN 0022-2623

Abstract

Protein kinase C (PKC) isotypes have emerged as a key novel target for the blockade of early T-cell activation. Herein, we report on the structure-activity relationship as well as the detailed physicochemical and in vivo pharmacokinetic properties of Sotrastaurin (AEB071, 1), a novel maleimide-based PKC inhibitor. The selective uptake of Sotrastaurin into lymphatic tissues might contribute to its in vivo efficacy and favorable therapeutic safety margin. Sotrastaurin is the first PKC inhibitor to show beneficial effects in patients suffering from psoriasis or to prevent graft rejection in transplanted patients in Phase II clinical trials.

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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/4420

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