Ligand-based targeting
Conventional chemotherapeutic agents do not preferentially localize at the site of disease, which may cause unnecessary toxicity and prevent escalation to therapeutic active regimens.
Philochem uses state-of-the-art technologies technologies to discover and develop novel therapeutics based on small organic ligands, cyclic peptides, and antibody fragments.
The approach crucially relies on the identification of accessible markers of disease and on the discovery of high affinity ligands, which facilitate pharmacodelivery applications.
Philochem develops product candidates, validates them in relevant models of disease and moves the most promising agents to clinical trials. While most activity are focused on oncology, the potential of Philochem’s approach extends to other disease areas, including chronic inflammation.
References
Molecular Evolution of Multivalent OncoFAP Derivatives with Enhanced Tumor Uptake and Prolonged Tumor Retention
Galbiati et al. (2024) J Med Chem. 67(15):13392
Preclinical Evaluation of 177Lu-OncoFAP-23, a Multivalent FAP-Targeted Radiopharmaceutical Therapeutic for Solid Tumors
Galbiati et al. (2024) J Nucl Med, 65(10):1604
In vivo activation of FAP-cleavable small molecule-drug conjugates for the targeted delivery of camptothecins and tubulin poisons to the tumor microenvironment
Bocci et al. (2024) J Control Release, 367:779
Targeted delivery of tumor necrosis factor in combination with CCNU induces a T cell–dependent regression of glioblastoma
Look et al. (2023) Sci Transl Med 15(697):eadf2281
Tumor-Targeted Interleukin 2 Boosts the Anticancer Activity of FAP-Directed Radioligand Therapeutics
Galbiati et al. (2023) J Nucl Med, 64(12):1934
Fibroblast Activation Protein Triggers Release of Drug Payload from Non-internalizing Small Molecule Drug Conjugates in Solid Tumors
Zana et al,. (2022), Clin Cancer Res CCR-22-1788
Backhaus et al. (2021) Eur J Nucl Med Mol Imaging, 10.21203/rs.3.rs-969176/v1
An ultra-high-affinity small organic ligand of fibroblast activation protein for tumor-targeting applications
Millul et al. (2021) PNAS, 118, 16, e2101852118
Enhanced Therapeutic Activity of Non-Internalizing Small-Molecule-Drug Conjugates Targeting Carbonic Anhydrase IX in Combination with Targeted Interleukin-2
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Wichert et al. (2015) Nat Chem, 7, 241-9
A Small-Molecule Drug Conjugate for the Treatment of Carbonic Anhydrase IX Expressing Tumors
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Interfering with pH regulation in tumours as a therapeutic strategy
Neri and Supuran (2011) Nat Rev Drug Discov, 10, 767-77
Tumour vascular targeting
Neri and Bicknell (2005) Nat Rev Cancer, 5, 436-46