Ultra-high performance liquid chromatography tandem mass spectrometric method for the determination of tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and endoxifen in dried blood spots--development, validation and clinical application during breast cancer adjuvant therapy

Talanta. 2015 Jan:132:775-84. doi: 10.1016/j.talanta.2014.10.040. Epub 2014 Oct 29.

Abstract

A LC-MSMS method for the simultaneous determination of tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and endoxifen in dried blood spots samples was developed and validated. The method employs an ultrasound-assisted liquid extraction and a reversed phase separation in an Acquity(®) C18 column (150×2.1 mm, 1.7 µm). Mobile phase was a mixture of formic acid 0.1% (v/v) pH 2.7 and acetonitrile (gradient from 60:40 to 50:50, v/v). Total analytical run time was 8 min. Precision assays showed CV % lower than 10.75% and accuracy in the range 94.5 to 110.3%. Mean analytes recoveries from DBS ranged from 40% to 92%. The method was successfully applied to 91 paired clinical DBS and plasma samples. Dried blood spots concentrations were highly correlated to plasma, with rs>0.83 (P<0.01). Median estimated plasma concentrations after hematocrit and partition factor adjustment were: TAM 123.3 ng mL(-1); NDT 267.9 ng mL(-1), EDF 10.0 ng mL(-1) and HTF 1.3 ng mL(-1,) representing in average 98 to 104% of the actually measured concentrations. The DBS method was able to identify 96% of patients with plasma EDF concentrations below the clinical threshold related to better prognosis (5.9 ng mL(-1)). The procedure has adequate analytical performance and can be an efficient tool to optimize adjuvant breast cancer treatment, especially in resource limited settings.

Keywords: 4-Hydroxytamoxifen; Dried blood spot; Endoxifen; LC–MS/MS; N-desmethyltamoxifen; Tamoxifen.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Agents, Hormonal / administration & dosage
  • Antineoplastic Agents, Hormonal / blood*
  • Biotransformation
  • Breast Neoplasms / blood*
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / pathology
  • Chromatography, High Pressure Liquid / methods
  • Dried Blood Spot Testing / standards*
  • Drug Monitoring
  • Female
  • Humans
  • Limit of Detection
  • Liquid-Liquid Extraction
  • Middle Aged
  • Sonication
  • Tamoxifen / administration & dosage
  • Tamoxifen / analogs & derivatives*
  • Tamoxifen / blood*
  • Tandem Mass Spectrometry

Substances

  • Antineoplastic Agents, Hormonal
  • Tamoxifen
  • afimoxifene
  • 4-hydroxy-N-desmethyltamoxifen
  • N-desmethyltamoxifen