Pharmacodynamic model of topotecan-induced time course of neutropenia

Clin Cancer Res. 2001 Aug;7(8):2301-8.

Abstract

Pharmacodynamic measures of neutropenia, such as absolute neutrophil count at nadir and neutrophil survival fraction, may not reflect the overall time course of neutropenia. We developed a pharmacokinetic-pharmacodynamic model to describe and quantify the time course of neutropenia after administration of topotecan to children and to compare this with nonhuman primates (NHPs) as a potential preclinical model of neutropenia. Topotecan was administered as a 30-min infusion daily for 5 days, repeated every 21 days. As part of a Phase I Pediatric Oncology Group study, topotecan was administered at 1.4 and 1.7 mg/m(2)/day without filgrastim (POG), and at 1.7, 2, and 2.4 mg/m(2)/day with filgrastim (POG+G). In NHPs, topotecan was administered at 5, 10, and 20 mg/m(2)/day without filgrastim. A pharmacokinetic-pharmacodynamic model was fit to profiles of topotecan lactone plasma concentrations and neutrophil survival fraction from cycle 1 and used to calculate topotecan lactone area under the plasma concentration-versus-time curve from 0 to 120 h (AUC(LAC)) and the area between the baseline and treatment-related neutrophil survival fraction (ABC) from 0 to 700 h. The mean +/- SD neutrophil survival fraction at nadir for the POG, POG+G, and NHP groups was 0.12 +/- 0.09, 0.11 +/- 0.17, and 0.09 +/- 0.08, respectively (P > 0.05). The mean +/- SD for the ratio of ABC to AUC(LAC) for the POG and NHP groups was 1.02 +/- 0.38 and 0.16 +/- 0.09, respectively (P < 0.05). The model estimate of ABC and the ratio of ABC to AUC(LAC) in children and NHPs may better reflect sensitivity to chemotherapy-induced neutropenia.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Area Under Curve
  • Child
  • Child, Preschool
  • Clinical Trials, Phase I as Topic
  • Disease Models, Animal
  • Female
  • Filgrastim
  • Granulocyte Colony-Stimulating Factor / administration & dosage
  • Humans
  • Male
  • Metabolic Clearance Rate
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Neutropenia / chemically induced
  • Neutropenia / metabolism
  • Neutropenia / pathology*
  • Neutrophils / drug effects
  • Recombinant Proteins
  • Time Factors
  • Topoisomerase I Inhibitors
  • Topotecan / administration & dosage
  • Topotecan / adverse effects
  • Topotecan / pharmacokinetics*

Substances

  • Recombinant Proteins
  • Topoisomerase I Inhibitors
  • Granulocyte Colony-Stimulating Factor
  • Topotecan
  • Filgrastim