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Publications

Journal Article Ahead of print

PubMed: 42012405 DOI: 10.1021/acs.jmedchem.5c03817

SPECT/NIR Fluorescence Bimodal Use of Aza-BODIPY Probe Coupled with Cetuximab for Detection of Cancer: Proof of Concept on a Preclinical Head and Neck Squamous Cell Carcinoma Model.

J Med Chem

Authors: Christol Fabre, Amélie Godard, Malorie Privat, Mathieu Moreau, Fabien Dalonneau, Annika Sickinger, Olivier Maury, Pierre-Simon Bellaye, Bertrand Collin, Benoit Busser, Christian Adrien Righini, Christine Goze, Ewen Bodio, Lucie Sancey

Affiliations

  • University Grenoble Alpes, Inserm U1209 CNRS UMR 5309, Institute for Advanced Biosciences, F-38000 Grenoble, France.
  • Grenoble Alpes University Hospital (CHUGA), F-38043 Grenoble, France.
  • Institut de Chimie Moléculaire de l'Université de Bourgogne, ICMUB CNRS, UMR 6302, Université Bourgogne Europe, F-21000 Dijon, France.
  • CNRS, ENS de Lyon, CNRS, LCH, UMR 5182, F-69342 Lyon, France.
  • Université Bourgogne Europe, Centre Georges-François Leclerc, Unicancer, IMATHERA, UMR INSERM 1231, ICMUB CNRS, UMR 6302, HSP-Pathies Team, 21000 Dijon, France.
  • Institut Universitaire de France (IUF), F-75005 Paris, France.
  • Nantes Université, CNRS, CEISAM, UMR 6230, F-44000 Nantes, France.

Abstract

The study reports the synthesis and biological evaluation of [ 111In]In-WAZABY, a novel bimodal imaging probe based on a water-soluble NIR-II aza-BODIPY fluorophore. The platform enables the design of a bimodal imaging probe through conjugation to the anti-epithelial growth factor receptor (EGFR) antibody cetuximab and incorporation of a [ 111In]In-DOTA complex for single-photon emission computed tomography (SPECT) imaging. The resulting probe efficiently targets EGFR-expressing tumors in a murine model of head and neck squamous cell carcinoma (HSNCC). Multimodal imaging combining NIR-I/NIR-II fluorescence and SPECT revealed specific tumor accumulation and a strong spatial correlation between optical and SPECT signals, demonstrating that DOTA grafting does not compromise fluorophore behavior or in vivo stability. These results establish [ 111In]In-WAZABY as a promising dual-modality contrast agent for peroperative tumor localization and future fluorescence-guided surgery (FGS), enabling complementary deep-tissue and high-resolution imaging.

MeSH

Cells, Cetuximab, Carcinoma, Squamous Cell, Neoplasms, Squamous Cell Carcinoma Of Head And Neck, Tomography, Emission-Computed, Single-Photon