Survival efficacy of the PEGylated G-CSFs Maxy-G34 and neulasta in a mouse model of lethal H-ARS, and residual bone marrow damage in treated survivors

Health Phys. 2014 Jan;106(1):21-38. doi: 10.1097/HP.0b013e3182a4df10.

Abstract

In an effort to expand the worldwide pool of available medical countermeasures (MCM) against radiation, the PEGylated G-CSF (PEG-G-CSF) molecules Neulasta and Maxy-G34, a novel PEG-G-CSF designed for increased half-life and enhanced activity compared to Neulasta, were examined in a murine model of the Hematopoietic Syndrome of the Acute Radiation Syndrome (H-ARS), along with the lead MCM for licensure and stockpiling, G-CSF. Both PEG-G-CSFs were shown to retain significant survival efficacy when administered as a single dose 24 h post-exposure, compared to the 16 daily doses of G-CSF required for survival efficacy. Furthermore, 0.1 mg kg of either PEG-G-CSF affected survival of lethally-irradiated mice that was similar to a 10-fold higher dose. The one dose/low dose administration schedules are attractive attributes of radiation MCM given the logistical challenges of medical care in a mass casualty event. Maxy-G34-treated mice that survived H-ARS were examined for residual bone marrow damage (RBMD) up to 9 mo post-exposure. Despite differences in Sca-1 expression and cell cycle position in some hematopoietic progenitor phenotypes, Maxy-G34-treated mice exhibited the same degree of hematopoietic stem cell (HSC) insufficiency as vehicle-treated H-ARS survivors in competitive transplantation assays of 150 purified Sca-1+cKit+lin-CD150+cells. These data suggest that Maxy-G34, at the dose, schedule, and time frame examined, did not mitigate RBMD but significantly increased survival from H-ARS at one-tenth the dose previously tested, providing strong support for advanced development of Maxy-G34, as well as Neulasta, as MCM against radiation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Acute Radiation Syndrome / blood
  • Acute Radiation Syndrome / drug therapy*
  • Acute Radiation Syndrome / pathology
  • Acute Radiation Syndrome / physiopathology
  • Animals
  • Blood Cell Count
  • Body Weight / drug effects
  • Body Weight / radiation effects
  • Bone Marrow / drug effects*
  • Bone Marrow / pathology
  • Bone Marrow / physiopathology
  • Bone Marrow / radiation effects*
  • Bone Marrow Transplantation
  • Cell Cycle / drug effects
  • Cell Cycle / radiation effects
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Female
  • Filgrastim
  • Granulocyte Colony-Stimulating Factor / administration & dosage
  • Granulocyte Colony-Stimulating Factor / pharmacology*
  • Granulocyte Colony-Stimulating Factor / therapeutic use
  • Hematopoiesis / drug effects
  • Hematopoiesis / radiation effects
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / pharmacology*
  • Polyethylene Glycols / therapeutic use
  • Recombinant Proteins / administration & dosage
  • Recombinant Proteins / pharmacology
  • Recombinant Proteins / therapeutic use
  • Survival Analysis
  • Survivors
  • Time Factors

Substances

  • Maxy G34
  • Recombinant Proteins
  • Granulocyte Colony-Stimulating Factor
  • pegfilgrastim
  • Polyethylene Glycols
  • Filgrastim