A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule–Drug, Antibody–Drug, and Peptide–Drug Conjugates

Aureliano Zana,Claudia Puig-Moreno,Matilde Bocci,Ettore Gilardoni,Cesare Di Nitto,Lucrezia Principi,Domenico Ravazza,Giulia Rotta,Eleonora Prodi,Roberto De Luca,Dario Neri,Samuele Cazzamalli

Bioconjugate chemistry（2023）

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摘要

We present the first comparative evaluation of chemically defined antibody-drug conjugates (ADCs), small molecule-drug conjugates (SMDCs), and peptide-drug conjugates (PDCs) targeting and activated by fibroblast activation protein (FAP) in solid tumors. Both the SMDC (OncoFAP-Gly-Pro-MMAE) and the ADC (7NP2-Gly-Pro-MMAE) candidates delivered high amounts of active payload (i.e., MMAE) selectively at the tumor site, thus producing a potent antitumor activity in a preclinical cancer model.

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关键词

molecule–drug conjugates,peptide–drug,antibody–drug,protein-targeted

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