177Lu-CTR-FAPI

177Lu-CTR-FAPI is a radiopharmaceutical drug candidate designed for targeted cancer therapy. It consists of a fibroblast activation protein inhibitor (FAPI) conjugated to the radioactive isotope lutetium-177 (177Lu). The drug specifically targets fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts within the tumor microenvironment of many solid tumors, but minimally expressed in normal tissues. By binding to FAP, 177Lu-CTR-FAPI delivers localized beta radiation directly to the tumor stroma, resulting in cytotoxic effects on both stromal and adjacent tumor cells. This approach aims to improve therapeutic efficacy while minimizing off-target toxicity. Preclinical studies have demonstrated high FAP-binding affinity, favorable pharmacokinetics with prolonged tumor retention, and significant antitumor activity compared to monomeric or dimeric FAPI constructs[1]. The drug is being developed as a theranostic agent for use in both imaging and treatment of various solid tumors.

Other names

177Lu-covalent targeted radioligand-fibroblast activation protein inhibitor