2019
DOI: 10.2967/jnumed.118.224469
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Abstract: Cancer-associated fibroblasts constitute a vital subpopulation of the tumor stroma and are present in more than 90% of epithelial carcinomas. The overexpression of the serine protease fibroblast activation protein (FAP) allows a selective targeting of a variety of tumors by inhibitor-based radiopharmaceuticals (FAPIs). Of these compounds, FAPI-04 has been recently introduced as a theranostic radiotracer and demonstrated high uptake into different FAP-positive tumors in cancer patients. To enable the delivery o… Show more

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Cited by 292 publications
(243 citation statements)
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“…The lowest 68 Ga-FAPI uptake (average SUV max , 6) was observed in renal cell, differentiated thyroid, adenoid cystic, gastric, and pheochromocytoma cancer. The average SUV max of hepatocellular, colorectal, head-neck, ovarian, pancreatic, and prostate cancer was intermediate (SUV [6][7][8][9][10][11][12]. All tumor entities exhibited a high interindividual SUV variation (Fig.…”
Section: Quantifying 68 Ga-fapi Uptake In Primary Tumors and Metastatmentioning
confidence: 99%
See 1 more Smart Citation
“…The lowest 68 Ga-FAPI uptake (average SUV max , 6) was observed in renal cell, differentiated thyroid, adenoid cystic, gastric, and pheochromocytoma cancer. The average SUV max of hepatocellular, colorectal, head-neck, ovarian, pancreatic, and prostate cancer was intermediate (SUV [6][7][8][9][10][11][12]. All tumor entities exhibited a high interindividual SUV variation (Fig.…”
Section: Quantifying 68 Ga-fapi Uptake In Primary Tumors and Metastatmentioning
confidence: 99%
“…A biodistribution and initial dosimetry study of 68 Ga-FAP inhibitor (FAPI) PET/CT with 2 DOTA-containing ligands suggested that these tracers may expand and enrich the diagnostic cancer portfolio currently covered by 18 F-FDG (6). Moreover, the biodistribution suggested that 68 Ga-FAPI may be suitable for radioligand therapy (7). In view of the favorable initial results, 68 Ga-FAPI PET/CT was requested by various referring physicians on the basis of individual clinical indications.…”
mentioning
confidence: 99%
“…Other equally exciting nuclear theranostic approaches are emerging. The Heidelberg group has identified the fibroblast activation protein as a tumor stroma target (78) and has developed a series of quinolone-based fibroblast activation protein ligands (79). 68 Galabaled ligands accumulate with high specificity in target structures.…”
Section: Nuclear Theranosticsmentioning
confidence: 99%
“…Applications of these molecules cover both diagnosis and therapy. [24][25][26][27][28][29] First, a DOTA-FAPI conjugate using piperazine as linker (referred to as FAPI-02 in the original reference) was synthesized and characterized with respect to binding, internalization, and e ux in cells expressing human and murine FAP as well as CD26. PETimaging studies of HT-1080 tumor xenografts showed low [ 68 Ga]Ga-FAPI-02 accumulation in normal tissues and a rapid clearance from the blood via kidneys and bladder.…”
Section: Introductionmentioning
confidence: 99%
“…Several of these had improved imaging parameters, with FAPI-04, FAPI-21 and FAPI-46 being relevant examples. [25,26] These compounds also had low nanomolar FAP-a nity (IC 50 = 6.5 nM for FAPI-04, IC 50 = 6.7 nM for FAPI-21 and IC 50 = 13.5 nM for FAPI-46), higher tumor uptakes in vivo and longer tumor retention times. First PET/CT imaging studies of patients diagnosed with different tumor entities were performed with the 68 Gacompounds indicating high tumor uptake and low background in healthy organs.…”
Section: Introductionmentioning
confidence: 99%