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. 2022 May 25;12:854658. doi: 10.3389/fonc.2022.854658

Table 1.

FAPIs that have been used in clinical studies.

Tracer Chemical Structure Author and Year Tumor (Patients) Key Finding
FAPI-02 graphic file with name fonc-12-854658-g006.jpg Loktev et al. (16)
2018		 Metastasized breast cancer (one patient)
metastasized lung cancer (one patient)
metastasized pancreatic cancer (one patient)		 68Ga-FAPI-02 is seen to selectively accumulate in FAP-expressing tissue and to be significantly higher than18F-FDG in malignant lesions(SUVmax of 13.3);
unlike 18F-FDG, 68Ga-FAPI-02 shows no uptake in brain, spleen, or liver.
FAPI-04 graphic file with name fonc-12-854658-g007.jpg Lindner et al. (17)
2018		 Metastasized breast cancer
(two patients)		 FAPI-04 shows rapid internalization into FAP-positive tumors and fast clearance from the body, resulting in very fast accumulation at tumor sites (10 min after tracer administration); the effective tumor uptake after 24 h—100% higher for FAPI-04 than for FAPI-02.
FAPI-46 graphic file with name fonc-12-854658-g008.jpg Loktev et al. (18)
2019		 Various cancers
(eight patients)		 High intratumoral uptake of FAPI-46 already 10 min after administration;
demonstration of higher tumor uptake with FAPI-46 Than with FAPI-04.
FAPI-34 graphic file with name fonc-12-854658-g009.jpg Lindner et al. (19)
2020		 Metastasized ovarian cancer (one patient) and pancreatic cancer (one patient) 99mTc-FAPI-34 represents a powerful tracer for diagnostic scintigraphy, especially when PET imaging is not available.
FAPI-74 graphic file with name fonc-12-854658-g010.jpg Giesel et al. (20)
2021		 Lung cancer
(10 patients)		 The high contrast and low radiation burden compared with 18F-FDG; best correlation to CT-based target volumes occurred at an SUV of three-fold the background.
DOTA-2P(FAPI)2 graphic file with name fonc-12-854658-g011.jpg Zhao et al. (22)
2021		 Nasopharyngeal cancer, papillary thyroid cancer, and HCC
(three patients)		 Exhibits better in vivo pharmacokinetics and higher tumor uptake than FAPI alone; has a long retention time in the blood pool and shows higher physiological uptake in the thyroid and pancreas.
DOTA.SA.FAPI graphic file with name fonc-12-854658-g012.jpg Ballal et al. (27)
2021		 Various cancers
(54 patients)		 TBR was comparable to previously reported data for FAPI-04; there was an advantage in brain metastasis compared with 18F-FDG.
NOTA-FAPI-04
(FAPI-42) 		graphic file with name fonc-12-854658-g013.jpg Wang et al. (23)
2021		 Various cancers
(10 patients)		 No defluorination during the assay time; higher uptake and TBR in liver tumors and bone tumors compared with 68Ga-FAPI-04.