Pharmacokinetic and pharmacodynamic analysis of hyperthermic intraperitoneal oxaliplatin-induced neutropenia in subjects with peritoneal carcinomatosis

AAPS J. 2011 Mar;13(1):72-82. doi: 10.1208/s12248-010-9249-2. Epub 2011 Jan 6.

Abstract

The objective of this study was to characterize the pharmacokinetics and the time course of the neutropenia-induced by hyperthermic intraperitoneal oxaliplatin (HIO) after cytoreductive surgery in cancer patients with peritoneal carcinomatosis. Data from 30 patients who received 360 mg/m(2) of HIO following cytoreductive surgery were used for pharmacokinetic-pharmacodynamic (PK/PD) analysis. The oxaliplatin plasma concentrations were characterized by an open two-compartment pharmacokinetic model after first-order absorption from peritoneum to plasma. An oxaliplatin-sensitive progenitor cell compartment was used to describe the absolute neutrophil counts in blood. The reduction of the proliferation rate of the progenitor cells was modeled by a linear function of the oxaliplatin plasma concentrations. The typical values of oxaliplatin absorption and terminal half-lives were estimated to be 2.2 and 40 h, with moderate interindividual variability. Oxaliplatin reduced the proliferation rate of the progenitor cells by 18.2% per mg/L. No patient's covariates were related to oxaliplatin PK/PD parameters. Bootstrap and visual predictive check evidenced the model was deemed appropriate to describe oxaliplatin pharmacokinetics and the incidence and severity of neutropenia. A peritoneum oxaliplatin exposure of 65 and 120 mg·L/h was associated with a 20% and 33% incidence of neutropenia grade 4. The time course of neutropenia following HIO administration was well described by the semiphysiological PK/PD model. The maximum tolerated peritoneum oxaliplatin exposure is 120 mg L/h and higher exposures should be avoided in future studies. We suggest the prophylactic use of granulocyte colony stimulating factor for patients treated with HIO exposure higher than 65 mg L/h.

MeSH terms

  • Adult
  • Aged
  • Algorithms
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects*
  • Antineoplastic Agents / pharmacokinetics*
  • Carcinoma / drug therapy
  • Carcinoma / physiopathology*
  • Carcinoma / surgery
  • Chemistry, Pharmaceutical
  • Computer Simulation
  • Dose-Response Relationship, Drug
  • Drug Carriers
  • Female
  • Half-Life
  • Humans
  • Hyperthermia, Induced*
  • Infusions, Parenteral
  • Leukocyte Count
  • Male
  • Middle Aged
  • Models, Statistical
  • Neutropenia / chemically induced*
  • Neutropenia / physiopathology
  • Neutrophils / drug effects
  • Neutrophils / physiology
  • Organoplatinum Compounds / administration & dosage
  • Organoplatinum Compounds / adverse effects*
  • Organoplatinum Compounds / pharmacokinetics*
  • Oxaliplatin
  • Peritoneal Cavity
  • Peritoneal Neoplasms / drug therapy
  • Peritoneal Neoplasms / physiopathology*
  • Peritoneal Neoplasms / surgery
  • Software

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Organoplatinum Compounds
  • Oxaliplatin