title: Evaluation of the novel protein kinase C inhibitor sotrastaurin as immunosuppressive therapy after renal transplantation.
abstract: BACKGROUND
  The prevalence of acute renal allograft rejection has decreased substantially in past decades due to new and more specific immunosuppressive compounds but improvements in long-term graft function have not been achieved. There is a large need for new immunosuppressive agents that lack toxicity of current agents such as calcineurin inhibitors but show high synergistic efficiency in preventing rejection processes.
  
  
  METHODS
  This review summarizes data concerning the pharmacokinetics, pharmacodynamics and clinical efficacy of the new PKC inhibitor sotrastaurin with a focus on renal transplantation. The article contains information that has been presented at international transplant meetings and congresses and that has been published between 2006 and 2010. Additionally, current ongoing trials are described in detail.
  
  
  RESULTS
  Immunosuppressive regimens after kidney transplantation consist of a combination of several agents in order to minimize drug toxicity. Therefore, the reader is presented with the most up-to-date/current developments in sotrastaurin applications in Phase I and II trials with emphasis on data maintained from studies that combined sotrastaurin with established agents such as mycophenolic acid and tacrolimus.
  
  
  CONCLUSIONS
  Several trials are ongoing and planned to determine the optimal immunosuppressive regimen to benefit from sotrastaurin's distinct mechanism of action.
authors.affiliation: Med. Klinik mS Nephrologie, Universitätsmedizin Charité, Berlin, Germany. mareen.matz@charite.de
authors.forename: Mareen
authors.initials: M
authors.lastname: Matz
authors.forename: Marcel
authors.initials: M
authors.lastname: Naik
authors.forename: Mir-Farzin
authors.initials: MF
authors.lastname: Mashreghi
authors.forename: Petra
authors.initials: P
authors.lastname: Glander
authors.forename: Hans-H
authors.initials: HH
authors.lastname: Neumayer
authors.forename: Klemens
authors.initials: K
authors.lastname: Budde
mesh_terms: D065095:Calcineurin Inhibitors; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D016572:Cyclosporine / Q000494:pharmacology; D004341:Drug Evaluation; D004359:Drug Therapy, Combination; D064420:Drug-Related Side Effects and Adverse Reactions / Q000378:metabolism; D006084:Graft Rejection / Q000517:prevention & control*; D006801:Humans; D007166:Immunosuppressive Agents / Q000494:pharmacology*; D016030:Kidney Transplantation; D009173:Mycophenolic Acid / Q000493:pharmacokinetics; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D011758:Pyrroles / Q000493:pharmacokinetics*; D011799:Quinazolines / Q000493:pharmacokinetics*; D020123:Sirolimus / Q000494:pharmacology; D016559:Tacrolimus / Q000493:pharmacokinetics; D016896:Treatment Outcome
chemical_list: D065095:Calcineurin Inhibitors; D007166:Immunosuppressive Agents; D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D011799:Quinazolines; C543528:sotrastaurin; D016572:Cyclosporine; D011493:Protein Kinase C; D009173:Mycophenolic Acid; D020123:Sirolimus; D016559:Tacrolimus