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DRUG:

[177Lu]FAPI-46

i
Other names: FAPI-46, [177Lu]FAPI-46
Associations
Company:
Novartis
Drug class:
FAP inhibitor
Associations
4ms
In vitro and in vivo analyses of eFAP: a novel FAP-targeting small molecule for radionuclide theranostics and other oncological interventions. (PubMed, EJNMMI Radiopharm Chem)
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.
Preclinical • Journal
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FAP (Fibroblast activation protein, alpha)
|
[177Lu]FAPI-46
6ms
The Synergy of 177Lu-FAPI-046 with Tyrosine Kinase Inhibitor in a Sarcoma Patient-Derived Xenograft Mouse Model. (PubMed, Biomed J)
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.
Preclinical • Journal
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CASP3 (Caspase 3) • FAP (Fibroblast activation protein, alpha)
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FAP expression
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pazopanib • [177Lu]FAPI-46
almost3years
Head-to-head comparison of Ga-FAPI-46 and F-FDG PET/CT for evaluation of head and neck squamous cell carcinoma: a single-center exploratory study. (PubMed, J Nucl Med)
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.
Clinical • Journal • Head-to-Head
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
3years
Correlation of Ga-FAPi-46 PET biodistribution with FAP expression by immunohistochemistry in patients with solid cancers: a prospective translational exploratory study. (PubMed, J Nucl Med)
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.
Clinical • Journal
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
3years
Simultaneous FAPI PET/MRI Targeting the Fibroblast-Activation Protein for Breast Cancer. (PubMed, Radiology)
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..
Journal
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FAP (Fibroblast activation protein, alpha)
|
[177Lu]FAPI-46
3years
Fibroblast activation protein targeted therapy using [Lu]FAPI-46 compared with [Ac]FAPI-46 in a pancreatic cancer model. (PubMed, Eur J Nucl Med Mol Imaging)
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.
Preclinical • Journal
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
over3years
Initial clinical experience with Y-FAPI-46 radioligand therapy for advanced stage solid tumors: a case series of nine patients. (PubMed, J Nucl Med)
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.
Clinical • Journal
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
over3years
Fibroblast Activation Protein specific PET/CT imaging in fibrotic interstitial lung diseases and lung cancer: a translational exploratory study. (PubMed, J Nucl Med)
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.
Journal
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
over3years
Ga-68-FAPI as diagnostic tool in sarcoma: Data from the FAPI-PET prospective observational trial. (PubMed, J Nucl Med)
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.
Clinical • Observational data • Journal
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FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
4years
FAPI PET Prost: Prospective Exploratory Study of FAPi PET/CT in Prostate Cancer With Histopathology Validation (clinicaltrials.gov)
P1, N=30, Recruiting, Jonsson Comprehensive Cancer Center | Not yet recruiting --> Recruiting
Clinical • Enrollment open
|
FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
4years
68Ga-FAPi-46 PET/CT Scan in Imaging Patients With Sarcoma (clinicaltrials.gov)
P1, N=30, Recruiting, Jonsson Comprehensive Cancer Center | Not yet recruiting --> Recruiting
Clinical • Enrollment open
|
FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
over4years
68Ga-FAPi-46 PET/CT Scan in Imaging Patients With Sarcoma (clinicaltrials.gov)
P1, N=30, Not yet recruiting, Jonsson Comprehensive Cancer Center
Clinical • New P1 trial
|
FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46
over4years
Clinical • New P1 trial
|
FAP (Fibroblast activation protein, alpha)
|
FAP expression
|
[177Lu]FAPI-46