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A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule-Drug, Antibody-Drug, and Peptide-Drug Conjugates.
Zana, Aureliano; Puig-Moreno, Claudia; Bocci, Matilde; Gilardoni, Ettore; Di Nitto, Cesare; Principi, Lucrezia; Ravazza, Domenico; Rotta, Giulia; Prodi, Eleonora; De Luca, Roberto; Neri, Dario; Cazzamalli, Samuele.
Affiliation
  • Zana A; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Puig-Moreno C; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Bocci M; Swiss Federal Institute of Technology, Department of Chemistry and Applied Biosciences, CH-8093 Zürich, Switzerland.
  • Gilardoni E; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Di Nitto C; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Principi L; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Ravazza D; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Rotta G; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Prodi E; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • De Luca R; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Neri D; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
  • Cazzamalli S; Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Zürich, Switzerland.
Bioconjug Chem ; 34(7): 1205-1211, 2023 07 19.
Article in En | MEDLINE | ID: mdl-37399501
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.
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Full text: 1 Database: MEDLINE Main subject: Immunoconjugates / Neoplasms / Antineoplastic Agents Limits: Humans Language: En Journal: Bioconjug Chem Journal subject: BIOQUIMICA Year: 2023 Type: Article Affiliation country: Switzerland
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Full text: 1 Database: MEDLINE Main subject: Immunoconjugates / Neoplasms / Antineoplastic Agents Limits: Humans Language: En Journal: Bioconjug Chem Journal subject: BIOQUIMICA Year: 2023 Type: Article Affiliation country: Switzerland