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. 2025 Dec 15:131:118382.
doi: 10.1016/j.bmc.2025.118382. Epub 2025 Sep 24.

Antibody drug conjugates of echinomycin-based payloads

Thomas Nittoli  1 , Nurul Ansari  2 , Po-Cheng Yu  2 , Lisa Strong  2 , Pooja Yadav  2 , Nalini Sathyanarayan  2 , Grant Harradence  2 , Jerry Taylor  2 , Alex Coburn  2 , Pearce Curran  2 , Serena Carosso  2 , Erika Kovas  2 , William Olson  3
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Antibody drug conjugates of echinomycin-based payloads

Thomas Nittoli et al. Bioorg Med Chem. .

Abstract

Antibody drug conjugates (ADCs) based on the natural product echinomycin have been developed. By replacing unique and synthetically challenging functionality along with sidechain modifications and quinoxaline functionality, a variety of potent cytotoxic derivatives were discovered. The authors in this report employed the well-studied HER2 model system along with a MDR cell line to probe for drug resistance. The research resulted in potent quinoline/quinoxaline-based payloads that were further elaborated with linkers for conjugating to antibodies. Targeting and non-targeting ADCs yielded potent and selective conjugates.

Keywords: Antibody; Antibody drug conjugate; Echinomycin; HER2.

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Conflict of interest statement

Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Thomas Nittoli reports a relationship with Regeneron Pharmaceuticals Inc. that includes: equity or stocks. Thomas Nittoli has patent #WO2025117727 pending to Regeneron Pharmaceuticals, Inc. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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