A simple HPLC-UV method for the simultaneous quantification of gefitinib and erlotinib in human plasma

J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Aug 1;879(23):2345-50. doi: 10.1016/j.jchromb.2011.06.026. Epub 2011 Jun 22.

Abstract

Gefitinib and erlotinib are two oral tyrosine kinase inhibitors (TKI) approved for the treatment of advanced non-small cell lung cancer (NSCLC). Published methods for simultaneous analysis of erlotinib and gefitinib in plasma are exclusively based on mass spectrometry. The purpose of this study was to develop a simple and sensitive HPLC-UV method to simultaneously quantify these two TKI in plasma. Following liquid-liquid extraction, gefitinib, erlotinib and sorafenib (internal standard), were separated with gradient elution (on a C8+ Satisfaction(®) using a mobile phase of acetonitrile/20mM ammonium acetate pH 4.5). Samples were eluted at a flow rate of 0.4 ml/min throughout the 15-min run. Dual UV wavelength mode was used, with gefitinib and erlotinib monitored at 331 nm, and sorafenib at 249 nm. The calibration was linear in the range 20-1000 ng/ml and 80-4000 ng/ml for gefitinib and erlotinib, respectively. Inter- and intra-day imprecision were less than 7.2% and 7.6% for gefitinib and erlotinib, respectively. This analytical method was successfully applied to assess the steady state plasma exposure to these TKI in NSCLC patients. This simple, sensitive, accurate and cost-effective method can be used in routine clinical practice to monitor gefitinib or erlotinib concentrations in plasma from NSCLC patients.

Publication types

  • Evaluation Study

MeSH terms

  • Antineoplastic Agents / blood*
  • Antineoplastic Agents / therapeutic use
  • Carcinoma, Non-Small-Cell Lung / blood*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Chromatography, High Pressure Liquid / methods*
  • Erlotinib Hydrochloride
  • Gefitinib
  • Humans
  • Lung Neoplasms / blood*
  • Lung Neoplasms / drug therapy
  • Quinazolines / blood*
  • Quinazolines / therapeutic use
  • Spectrophotometry, Ultraviolet / methods*

Substances

  • Antineoplastic Agents
  • Quinazolines
  • Erlotinib Hydrochloride
  • Gefitinib