On October 19, 2022 Philogen S.p.A., a clinical-stage biotechnology company focused on the development of innovative medicines based on tumor targeting antibodies and small molecule ligands, reported the publication of a study in the peer-reviewed journal "Clinical Cancer Research" describing the development and the in vitro/vivo characterization of novel OncoFAP-based Small Molecule-Drug Conjugates (SMDCs) (Press release, Philogen, OCT 19, 2022, View Source [SID1234622177]). The study was conducted by scientists at Philochem AG, the wholly-owned Swiss subsidiary company of Philogen. The paper can be accessed from the Clinical Cancer Research website under the following link.
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Fibroblast Activation Protein (FAP) has recently emerged as a tumor-associated antigen with abundant and selective expression in the majority of human solid malignancies. OncoFAP is an ultra-high affinity small organic ligand with a picomolar dissociation constant. The targeting potential of OncoFAP has been validated in human patients with different types of cancers (e.g., esophageal, breast, hepatocellular, pancreatic) showing excellent selectivity for the tumor and low kidney uptake. OncoFAP was used as a modular component for generating SMDCs equipped with the cytotoxic payload Monomethyl Auristatin E (MMAE) and novel cleavable linkers that are rapidly and selectively cleaved by FAP. Different linkers were compared in vitro and in vivo for their kinetics of payload release using an advanced mass spectrometry-based quantification technology. OncoFAP-Gly-Pro-MMAE emerged as best-in-class product for the selective and prolonged release of MMAE payload to FAP-positive tumor lesions. OncoFAP-Gly-Pro-MMAE displayed excellent therapeutic performance in preclinical models of cancer even with a single administration. The results presented in the Clinical Cancer Research paper support clinical development of OncoFAP-Gly-Pro-MMAE.
Dario Neri, Chief Executive Officer of Philogen commented: "The study demonstrates the impressive tumortargeting and therapeutic performance of our novel Small Molecule Drug Conjugates targeting FAP. These novel products also benefit from the excellent imaging data collected so far with the OncoFAP ligand, which has been already administered to more than 60 cancer patients. We look forward to growing our small molecule clinical pipeline based on the OncoFAP delivery platform."
Samuele Cazzamalli, Head of Small Molecule Therapeutics of Philochem AG commented: "Our aim is to make OncoFAP-based therapies available to cancer patients. Companion diagnostics based on OncoFAP will allow us to select individuals that will most likely benefit from therapies based on FAP-targeted Small Molecule Therapeutics. We look forward to progressing the development of this important technology with the potential of benefitting millions of patients."