FAPI-2 (TFA)

FAPI-2 TFA is a type of small molecule fibroblast activation protein inhibitor (FAPI) that targets the fibroblast activation protein (FAP) and has an inhibitory effect. This specific targeting ability makes FAPI-2 TFA an effective tumor imaging agent, which can be used in cancer research. FAPI-2 TFA can be used to synthesize 68Ga-FAPI-2 (a PET tracer)[1][2][3][4].

[1]Giesel FL, et al. 68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers. J Nucl Med. 2019 Mar;60(3):386-392.|[2]Moon ES, et al. Fibroblast Activation Protein (FAP) targeting homodimeric FAP inhibitor radiotheranostics: a step to improve tumor uptake and retention time. Am J Nucl Med Mol Imaging. 2021 Dec 15;11(6):476-491.|[3]Li M, et al. Clinical summary of fibroblast activation protein inhibitor-based radiopharmaceuticals: cancer and beyond. Eur J Nucl Med Mol Imaging. 2022 Jul;49(8):2844-2868. doi: 10.1007/s00259-022-05706-y. Epub 2022 Jan 31. Erratum in: Eur J Nucl Med Mol Imaging. 2022 Jul;49(8):3007.|[4]Sanjana Ballal, et al. First-in-Human Experience With 177Lu-DOTAGA.(SA.FAPi)2 Therapy in an Uncommon Case of Aggressive Medullary Thyroid Carcinoma Clinically Mimicking as Anaplastic Thyroid Cancer. Clin Nucl Med. 2022 Jun 1;47(6):e444-e445.