Drug intelligence / Profile preview

177Lu-HX02

Development stage
Unknown
Lead developer
Hexin Pharmaceutical Technology
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

177Lu-HX02 is a therapeutic radiopharmaceutical developed by Hexin Suzhou Pharmaceutical Technology for the treatment of advanced solid tumors. It consists of the beta-emitting radioisotope Lutetium-177 ($^{177}$Lu) conjugated to a high-affinity ligand (HX02) that specifically targets Fibroblast Activation Protein (FAP). FAP is a cell-surface serine protease that is highly overexpressed on cancer-associated fibroblasts (CAFs) within the stroma of various epithelial cancers, including pancreatic, colorectal, and breast cancers, while showing minimal expression in healthy adult tissues. Upon intravenous administration, 177Lu-HX02 selectively accumulates in the tumor microenvironment by binding to FAP-expressing cells. The localized emission of beta particles from the Lutetium-177 payload induces double-stranded DNA breaks and subsequent apoptosis in both the stromal fibroblasts and adjacent malignant cells via the bystander effect, thereby disrupting the tumor-supportive stroma and directly eliminating tumor cells.

Other names
Lutetium (177Lu) HX02177Lu-HX02 injection
02

Targets

FAP (Fibroblast activation protein alpha)

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