Phase I study of the safety and pharmacokinetics of plerixafor in children undergoing a second allogeneic hematopoietic stem cell transplantation for relapsed or refractory leukemia

Biol Blood Marrow Transplant. 2014 Aug;20(8):1224-8. doi: 10.1016/j.bbmt.2014.04.020. Epub 2014 Apr 23.

Abstract

The safety, pharmacokinetics, and biological effect of plerixafor in children as part of a conditioning regimen for chemo-sensitization in allogeneic hematopoietic stem cell transplantation (HSCT) have not been studied. This is a phase I study of plerixafor designed to evaluate its tolerability at dose of .24 mg/kg given intravenously on day -4 (level 1); day -4 and day -3 (level 2); or day -4, day -3, and day -2 (level 3) in combination with fludarabine, thiotepa, melphalan, and rabbit antithymocytic globulin for a second allogeneic HSCT in children with refractory or relapsed leukemia. Immunophenotype analysis was performed on blood and bone marrow before and after plerixafor administration. Twelve patients were enrolled. Plerixafor at all 3 levels was well tolerated without dose-limiting toxicity. Transient gastrointestinal side effects of National Cancer Institute-grade 1 or 2 in severity were the most common adverse events. The area under the concentration-time curve increased proportionally to the dose level. Plerixafor clearance was higher in males and increased linearly with body weight and glomerular filtration rate. The clearance decreased and the elimination half-life increased significantly from dose level 1 to 3 (P < .001). Biologically, the proportion of CXCR4(+) blasts and lymphocytes both in the bone marrow and peripheral blood increased after plerixafor administration.

Keywords: Allogeneic; Children; Plerixafor; Stem cell transplantation.

Publication types

  • Clinical Trial, Phase I
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzylamines
  • Biomarkers, Pharmacological
  • Cyclams
  • Female
  • Hematopoietic Stem Cell Transplantation / adverse effects
  • Heterocyclic Compounds / administration & dosage
  • Heterocyclic Compounds / pharmacokinetics*
  • Heterocyclic Compounds / therapeutic use*
  • Humans
  • Immunophenotyping
  • Leukemia / drug therapy
  • Leukemia / etiology*
  • Male
  • Recurrence
  • Transplantation Conditioning
  • Transplantation, Homologous
  • Treatment Outcome

Substances

  • Benzylamines
  • Biomarkers, Pharmacological
  • Cyclams
  • Heterocyclic Compounds
  • plerixafor