Rofapitide tetraxetan (FAP-2286) is a potent and selective FAP-binding peptide with a mean IC50 value of 2.7 nM for binding to FAP. Rofapitide tetraxetan can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan has antitumor activity[1].
FAP-2286, a fibroblast activation protein (FAP)-binding peptidic macrocycle coupled to the radionuclide chelator DOTA. FAP-2286 has potent affinity to human FAP protein with a Kd of 1.1 nM. FAP-2286, a tumor imaging agent, is a useful tool for the research of positron emission tomography (PET). FAP-2286 has antitumor activity[1][2].
Rofapitide tetraxetan (30 MBq/nmol for intravenous injection) accumulated atably maintained in the tumors of HEK-FAP tumor-bearing mice[1].
| Animal Model: | HEK-FAP tumor-bearing mice[1] |
| Dosage: | 30 MBq/nmol |
| Administration: | Intravenous injection (i.v.) |
| Result: | Increased tumor-to-kidney (T/K) ratio with the highest differential uptake of 7.5 T/K obtained at 48 h post injection.
Maintained accumulation at 3 h after injection with 10.8 ID/g.
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[1]. Dirk Zboralski, et al. Comparative Biodistribution and Radiotherapeutic Efficacy of the Fibroblast Activation Protein (FAP)-Targeting Agents FAP-2286 and FAPI-46.[2]. Richard P Baum, et al. Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177 Lu-FAP-2286: First-in-Humans Results. J Nucl Med. 2022 Mar;63(3):415-423.