68Ga-DOTA-2P(FAPI)2

68Ga-DOTA-2P(FAPI)2 is an investigational radiopharmaceutical diagnostic imaging agent designed for positron emission tomography (PET). It consists of a dimeric structure of a fibroblast activation protein inhibitor (FAPI) ligand, conjugated to the chelator DOTA and labeled with the positron-emitting radioisotope Gallium-68. The agent specifically targets Fibroblast Activation Protein (FAP), a type II transmembrane serine protease that is highly overexpressed on cancer-associated fibroblasts (CAFs) within the stroma of various solid tumors, while having low expression in normal tissues. The dimeric '2P' configuration is engineered to provide bivalent binding, which enhances binding affinity and prolongs tumor retention time compared to traditional monomeric FAPI tracers like FAPI-04 or FAPI-46. This improved pharmacokinetic profile is intended to increase the sensitivity and diagnostic accuracy of PET/CT imaging for detecting primary and metastatic lesions in cancers such as gastric, pancreatic, and colorectal malignancies.

Other names

Gallium Ga 68 DOTA-2P(FAPI)268Ga-labeled FAPI dimer68Ga-DOTA-FAPI dimer