A Small-Molecule Drug Conjugate Targeting FAP Exhibits Potent Activity in Dogs with Spontaneous Tumors
Year: 2026
Type: article
Abstract: Antibody-drug conjugates have transformed the treatment of cancer, yet their clinical utility can be limited by suboptimal tumor penetration, complex manufacturing, and safety concerns. Replacing antibodies with low-molecular-weight ligands enables the generation of small molecule-drug conjugates with enhanced tumor-targeting performance. Here, we report the results of a proof-of-concept study in canine cancer patients with OncoFAP glidotin, a small molecule-based targeted cytotoxic directed against Fibroblast Activation Protein. OncoFAP glidotin was evaluated in a dose-escalation trial in eight client-owned pet dogs bearing spontaneous FAP-positive tumors. The agent displayed an excellent safety profile, with no severe treatment-related adverse events. Six (75%) patients responded to the therapy. A tumor volume reduction of up to ∼88% in target lesions was observed on whole-body computed tomography, after only 4 weeks of treatment. These findings support further translational development activities of OncoFAP glidotin for both human and veterinary cancer patients.
Source: Journal of Medicinal Chemistry
Authors: Andrea Galbiati, Paola Roccabianca, Silvia Dell’Aere, Matilde Bocci, Luigi Auletta, Roberta Ferrari, Alessandra Ubiali, Elisa M. Gariboldi, Emanuele Marsala, Pinuccia Faviana, Francesco Bartoli, Beatrice Zoanni, Ettore Gilardoni, Maurizio Longo, Dario Neri, Damiano Stefanello, Samuele Cazzamalli
Language: English
Subfield: Oncology
Field: Medicine
Domain: Health Sciences
Open Access status: green
OpenAlex ID: W7161385785