Sotrastaurin in calcineurin inhibitor-free regimen using everolimus in de novo kidney transplant recipients

Am J Transplant. 2013 Jul;13(7):1757-68. doi: 10.1111/ajt.12255. Epub 2013 May 9.

Abstract

Sotrastaurin, a novel selective protein-kinase-C inhibitor, inhibits early T cell activation via a calcineurin-independent pathway. Efficacy and safety of sotrastaurin in a calcineurin inhibitor-free regimen were evaluated in this two-stage Phase II study of de novo kidney transplant recipients. Stage 1 randomized 131 patients (2:1) to sotrastaurin 300 mg or cyclosporine A (CsA). Stage 2 randomized 180 patients (1:1:1) to sotrastaurin 300 or 200 mg or CsA. All patients received basiliximab, everolimus (EVR) and prednisone. Primary endpoint was composite efficacy failure rate of treated biopsy-proven acute rejection, graft loss, death or lost to follow-up. Main safety assessment was estimated glomerular filtration rate (eGFR) by MDRD-4 at Month 12. Composite efficacy failure rates at 12 months were higher in sotrastaurin arms (Stage 1: 16.5% and 10.9% for sotrastaurin 300 mg and CsA; Stage 2: 27.2%, 34.5% and 19.4% for sotrastaurin 200 mg, 300 mg and CsA). eGFR was significantly better in sotrastaurin groups versus CsA at most time points, except at 12 months. Gastrointestinal and cardiac adverse events were more frequent with sotrastaurin. Higher treatment discontinuation, deaths and graft losses occurred with sotrastaurin 300 mg. Sotrastaurin combined with EVR showed higher efficacy failure rates and some improvement in renal allograft function compared to a CsA-based therapy.

Publication types

  • Clinical Trial, Phase II
  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Adult
  • Antineoplastic Agents
  • Biopsy
  • Calcineurin Inhibitors
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Everolimus
  • Female
  • Follow-Up Studies
  • Glomerular Filtration Rate
  • Graft Rejection / drug therapy*
  • Graft Rejection / pathology
  • Graft Rejection / physiopathology
  • Humans
  • Immunosuppressive Agents / administration & dosage
  • Kidney / pathology
  • Kidney / physiopathology
  • Kidney Transplantation*
  • Male
  • Middle Aged
  • Protein Kinase Inhibitors / administration & dosage
  • Pyrroles / administration & dosage*
  • Quinazolines / administration & dosage*
  • Retrospective Studies
  • Sirolimus / administration & dosage
  • Sirolimus / analogs & derivatives*
  • Transplantation, Homologous
  • Treatment Outcome

Substances

  • Antineoplastic Agents
  • Calcineurin Inhibitors
  • Immunosuppressive Agents
  • Protein Kinase Inhibitors
  • Pyrroles
  • Quinazolines
  • sotrastaurin
  • Everolimus
  • Sirolimus