The caspase inhibitor IDN-6556 (PF3491390) improves marginal mass engraftment after islet transplantation in mice

Surgery. 2011 Jul;150(1):48-55. doi: 10.1016/j.surg.2011.02.023. Epub 2011 May 18.

Abstract

Background: Islet transplantation has become a viable option for selected type 1 diabetic patients; however, a significant portion need to return to exogenous insulin. The predominant factors include impaired islet engraftment and early islet loss. Caspase inhibition is a potent way to improve islet engraftment, but all tested compounds so far have not been clinically relevant. IDN-6556 (PF3491390) has already been used clinically and can be delivered orally with high portal vein concentrations.

Methods: Mice were given a marginal mass islet graft of either mouse or human islets and treated with either IDN-6556 (10 or 20 mg/kg ip bid) or vehicle and followed for diabetes reversal. At 1 month post-transplant, mice were subjected to a glucose tolerance test and an assessment of graft mass. In separate experiments, human islets were cultured with IDN-6556 or vehicle to assess for islet survival and viability.

Results: In both syngeneic mouse islets and human islets transplanted into immunodeficient mice, IDN-6556 (20 mg/kg) given for 7 days post-transplant led to a significantly enhanced rate of diabetes reversal as compared to vehicle. In addition, mice receiving caspase inhibitor displayed improved glucose tolerance and graft survival at the 1-month point. We also found protective effects in vitro for islet viability and marked reduction in apoptosis in vivo.

Conclusion: Taken together, these results demonstrate the effectiveness of caspase inhibition with IDN-6556 on islet transplantation and in particular islet engraftment and survival.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Blood Glucose / metabolism
  • Caspase Inhibitors*
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Diabetes Mellitus, Experimental / blood
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / surgery
  • Glucose Tolerance Test
  • Graft Enhancement, Immunologic / methods*
  • Graft Survival / drug effects
  • Humans
  • Islets of Langerhans Transplantation* / pathology
  • Islets of Langerhans Transplantation* / physiology
  • Mice
  • Mice, Inbred BALB C
  • Mice, Knockout
  • Pentanoic Acids / pharmacology*
  • Transplantation, Heterologous
  • Transplantation, Isogeneic

Substances

  • 3-(2-(2-tert-butylphenylaminooxalyl)aminopropionylamino)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
  • Blood Glucose
  • Caspase Inhibitors
  • Cysteine Proteinase Inhibitors
  • Pentanoic Acids