Value of in vitro models for the assessment of drug-induced haematotoxicity

Therapie. 2004 Nov-Dec;59(6):607-10. doi: 10.2515/therapie:2004105.

Abstract

Background: A new antipsychotic compound induced unexpected red cell hypoplasia (reticulocytopenia, red marrow hypoplasia) in rats dosed orally for 7 days.

Materials and methods: Since an erythropoietin-mediated pathogenesis was excluded, in vitro tests on rat and human bone marrow cells were performed with measurement of formation of late erythroid (CFU-E) and granulocyte-macrophage (CFU-GM) colony-forming units after incubation with the drug. CFU-E together with growth factors were cultured for 2 days (rat) or 7 days (human) and CFU-GM was cultured for 7 days (rat) or 10 days (human).

Results: The drug induced inhibition of erythroid progenitors and myeloid progenitors for both species from 3 x 10(-5) mol/L, with the concentration inhibiting the growth of 50% (IC50) consistent with drug plasma levels measured in rats.

Conclusion: These cloning assays on rat bone-marrow cells were shown to be adequate models for determining the haematotoxicity of the agent and to be predictive of human toxicity. With only a small amount of compound required, they can be used as screening tools to detect haematotoxic potential of candidate drugs.

MeSH terms

  • Animals
  • Antipsychotic Agents / toxicity
  • Bone Marrow Cells / physiology
  • Cells, Cultured
  • Colony-Forming Units Assay
  • Erythroid Precursor Cells / drug effects
  • Erythropoietin / physiology
  • Hematologic Diseases / chemically induced*
  • Hematologic Diseases / diagnosis*
  • Humans
  • Models, Biological
  • Rats
  • Risk Assessment
  • Stem Cells / physiology

Substances

  • Antipsychotic Agents
  • Erythropoietin