Skip to main content
Go to the home page of the European Commission (opens in new window)
English en
CORDIS - EU research results
CORDIS

Dual-targeted KetoFAPI Conjugates for Tumor-Selective Bimodal Therapy in Triple-Negative Breast Cancer

Project description

A dual-action targeted therapy for triple-negative breast cancer

Triple-negative breast cancer is one of the most aggressive and difficult-to-treat cancer subtypes, with limited therapeutic options and poor survival rates. A protein called fibroblast activation protein is highly expressed in the tumour microenvironment but is largely absent from healthy tissue, making it an attractive therapeutic target. With the support of the Marie Skłodowska-Curie Actions programme, the BiFAP project aims to develop a single platform that combines chemotherapy and radionuclide therapy. To achieve this dual-targeting strategy, researchers propose to design targeted conjugates based on novel small molecules with exceptionally long tumour residence. The approach will be validated in organoid models and preclinical mouse studies, hoping to achieve enhanced tumour selectivity and reduced toxic side effects.

Objective

Triple-negative breast cancer (TNBC) remains one of the most aggressive subtypes of breast cancer, with limited therapeutic options and a poor prognosis. To offer dearly needed new treatment perspectives, we want to target fibroblast activation protein (FAP), a protease that is highly expressed on cancer-associated fibroblasts (CAFs) in tumors but negligible in most healthy tissue. Building on this rationale, the host institution has pioneered novel ketoFAPIs, small-molecule FAP inhibitors with exceptionally long tumor residence times, providing a unique opportunity to design advanced drug delivery platforms.
This project will exploit the unique properties of ketoFAPIs to design bimodal conjugates that combine chemotherapy and radionuclide therapy in a single, tumor-targeted platform. These conjugates will integrate: (i) a ketoFAPI as the primary targeting moiety, (ii) a DOTAGA chelator for radionuclide labeling, and (iii) a cleavable linker for selective intratumoral release of potent chemotherapeutics such as MMAE or SN-38. To further enhance tumor selectivity and reduce bone marrow toxicity, a dual-targeting strategy will be pursued by adding folic acid as a second tumor-binding ligand. The project is structured into three objectives: 1) synthesis and characterization of Type I and II conjugates, 2) in vitro validation of efficacy and selectivity in TNBC organoid models, 3) in vivo evaluation of biodistribution, tumor uptake, and bone marrow safety in TNBC mouse models.
By integrating long-residence FAP targeting with dual-modality therapy and dual-ligand selectivity, this research introduces a first-in-class therapeutic strategy for TNBC. Expected outcomes are optimized conjugates with enhanced tumor selectivity, reduced hematological toxicity, and improved therapeutic potential. Aligned with the EU’s Beating Cancer Plan, this project directly addresses the need for innovative, tumor-targeted therapies to improve cancer patient survival and quality of life.

Fields of science (EuroSciVoc)

Keywords

Programme(s)

Topic(s)

Funding Scheme

HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships

See all projects funded under this funding scheme

Call for proposal

(opens in new window) HORIZON-MSCA-2025-PF

See all projects funded under this call

Coordinator

UNIVERSITEIT ANTWERPEN
Net EU contribution
€ 216 240,00
Address
PRINSSTRAAT 13
2000 Antwerpen
Belgium
Region
Vlaams Gewest Prov. Antwerpen Arr. Antwerpen
Activity type
Higher or Secondary Education Establishments
Links
Total cost
No data