Utility of 18F-fluoroestradiol (18F-FES) PET/CT imaging as a pharmacodynamic marker in patients with refractory estrogen receptor-positive solid tumors receiving Z-endoxifen therapy

Frank I. Lin, E. M. Gonzalez, S. Kummar, K. Do, J. Shih, S. Adler, K. A. Kurdziel, A. Ton, B. Turkbey, P. M. Jacobs, S. Bhattacharyya, A. P. Chen, J. M. Collins, J. H. Doroshow, P. L. Choyke, M. L. Lindenberg

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

Background: Z-endoxifen is the most potent of the metabolites of tamoxifen, and has the potential to be more effective than tamoxifen because it bypasses potential drug resistance mechanisms attributable to patient variability in the expression of the hepatic microsomal enzyme CYP2D6. 18F-FES is a positron emission tomography (PET) imaging agent which selectively binds to estrogen receptor alpha (ER-α) and has been used for non-invasive in vivo assessment of ER activity in tumors. This study utilizes 18F-FES PET imaging as a pharmacodynamic biomarker in patients with ER+ tumors treated with Z-endoxifen. Methods: Fifteen patients were recruited from a parent therapeutic trial of Z-endoxifen and underwent imaging with 18F-FES PET at baseline. Eight had positive lesions on the baseline scan and underwent follow-up imaging with 18F-FES 1–5 days post administration of Z-endoxifen. Results: Statistically significant changes (p = 0.0078) in standard uptake value (SUV)-Max were observed between the baseline and follow-up scans as early as 1 day post drug administration. Conclusion: F-FES PET imaging could serve as a pharmacodynamic biomarker for patients treated with ER-directed therapy.

Original languageEnglish (US)
Pages (from-to)500-508
Number of pages9
JournalEuropean Journal of Nuclear Medicine and Molecular Imaging
Volume44
Issue number3
DOIs
StatePublished - Mar 1 2017
Externally publishedYes

Keywords

  • F-FES
  • Fluoroestradiol
  • Pharmacodynamic marker
  • Positron emission tomography (PET)
  • Z-endoxifen

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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