We present the first in vivo 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.
A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule-Drug, Antibody-Drug, and Peptide-Drug Conjugates / Zana, A.; Puig-Moreno, C.; Bocci, M.; Gilardoni, E.; Di Nitto, C.; Principi, L.; Ravazza, D.; Rotta, G.; Prodi, E.; De Luca, R.; Neri, D.; Cazzamalli, S.. - In: BIOCONJUGATE CHEMISTRY. - ISSN 1043-1802. - 34:7(2023), pp. 1205-1211. [10.1021/acs.bioconjchem.3c00244]
A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule-Drug, Antibody-Drug, and Peptide-Drug Conjugates
Rotta G.;Prodi E.;
2023-01-01
Abstract
We present the first in vivo 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione
