[177Lu]FAPI-46

[177Lu]Lu-FAPI-ET1 demonstrates that the endolysosomal trapping approach can be successfully implemented in FAP-targeted agents and achieve enhanced FAP-positive U-87MG tumor residualization. Although the decreased internalization rate and in vivo targeting of [177Lu]Lu-FAPI-ET1 compared to [177Lu]Lu-FAPI-46 and the ambiguity concerning FAP-mediated internalization efficacy due to targeting vector adduct formation are hurdles to the current implementation. Future approaches are focused on better characterizing FAP adduct formation and cellular trafficking to reveal new pathways to optimize the endolysosomal trapping approach for FAP-targeted agents.

The superior affinity and faster tumor accumulation of eFAP-6 over FAPI-46 makes it a suitable compound for radionuclide imaging. After further optimization, the eFAP series has great potential for various oncological interventions, including fluorescent-guided surgery and effective targeted radionuclide theranostics.

This study successfully demonstrated the reduction in FAP expression and suppression of tumor volume in sarcoma PDX following the combination therapy of 177Lu-FAPI-46 with Pazopanib.

FTV was greater than MTV (P < 0.05), but no significant differences were observed for the other parameters. Ga-FAPI-46 PET/CT showed good concordance and comparable diagnostic performance compared with F-FDG PET/CT for initial staging and recurrence detection in patients with HNSCC.

In this interim analysis of a prospective exploratory imaging trial, Ga-FAPi-46 PET biodistribution across multiple cancers strongly correlated with FAP tissue expression. These findings support further exploration of FAPi PET as a pan-cancer imaging biomarker for FAP expression and stratification tool for FAP- targeted therapies.

Purpose To evaluate the use of FAP inhibitor (FAPI) breast PET/MRI in assessing breast lesions and of FAPI whole-body scanning for lymph node (LN) and distant staging using the ligand gallium 68 (Ga)-FAPI-46..

This study suggested the possible application of FAPI radioligand therapy in FAP-expressing pancreatic cancer. Further evaluation is necessary to find the best radionuclide with shorter half-life, as well as the combination with therapies targeting tumour cells directly.

Low radiation doses to organs at risk suggest feasibility of repeat cycles of Y-FAPI-46. We observe signs of clinical activity, but further studies are warranted to determine efficacy and toxicity profile in a larger cohort.

Patients and PET-Scans of 15 patients with fILD and suspected LC were acquired 10, 60 and 180 minutes after the administration of 150-250 MBq of a Ga labelled FAPI tracer (FAPI-46)... FAPI-PET/CT imaging is a promising new imaging modality for fILD and LC. Its potential clinical value for monitoring and therapy evaluation of fILD should be investigated in future studies.

Novel radio-labelled FAP-Inhibitors (e.g. Ga-FAPI46) have shown high tumor uptake in positron emission tomography (PET) in sarcoma patients... We confirm an association of tumoral FAPI-PET uptake intensity and histopathological FAP expression in sarcoma patients. Further, using blinded reads and independent histopathological validation we report high PPV and sensitivity of FAPI-PET for sarcoma staging.

P1, N=30, Recruiting, Jonsson Comprehensive Cancer Center | Not yet recruiting --> Recruiting