2. Academic Validation
  3. Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis

  • J Med Chem. 2011 Sep 8;54(17):6028-39. doi: 10.1021/jm200469u.
Jürgen Wagner 1,  Peter von Matt,  Bernard Faller,  Nigel G Cooke,  Rainer Albert,  Richard Sedrani,  Hansjörg Wiegand,  Christian Jean,  Christian Beerli,  Gisbert Weckbecker,  Jean-Pierre Evenou,  Gerhard Zenke,  Sylvain Cottens
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland. juergen.wagner@novartis.com
PMID: 21797275 DOI: 10.1021/jm200469u
Abstract

Protein kinase C (PKC) isotypes have emerged as key targets for the blockade of early T-cell activation. Herein, we report on the structure-activity relationship and the detailed physicochemical and in vivo pharmacokinetic properties of sotrastaurin (AEB071, 1), a novel maleimide-based PKC Inhibitor currently in phase II clinical trials. Most notably, the preferred uptake of sotrastaurin into lymphoid tissues is an important feature, which is likely to contribute to its in vivo efficacy.

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