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lutetium Lu 177 AB-3PRGD2
- Development stage
- Unknown
- Lead developer
- Beijing Jiluntai Pharmaceutical
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intratumoral, Intravenous
01
Overview
Lutetium Lu 177 AB-3PRGD2 (also known as 177Lu-AB-3PRGD2 or 177Lu-JLT003) is an innovative, clinical-stage therapeutic radiopharmaceutical (radioligand therapy) designed to target integrin αvβ3-positive solid tumors. Developed by Beijing Jiluntai Pharmaceutical in collaboration with Peking Union Medical College Hospital and Peking University, the drug consists of a PEGylated cyclic RGD dimer (PRGD2) that specifically binds to integrin αvβ3, which is highly overexpressed on tumor cells and neovascular endothelial cells. To optimize its pharmacokinetic profile, the molecule incorporates an albumin-binding motif that extends its blood circulation half-life and enhances tumor accumulation. The targeting peptide is labeled with the beta-emitting radionuclide lutetium-177 (177Lu), which delivers localized cytotoxic radiation to destroy tumor cells. In clinical trials, lutetium Lu 177 AB-3PRGD2 has demonstrated promising efficacy and a manageable safety profile in patients with advanced metastatic solid tumors, including thyroid, breast, lung, and renal cancers. It is also being investigated for locoregional administration in glioblastoma multiforme.
- Other names
- 177Lu-3PRGD2177Lu-AB-3PRGD2[177Lu]Lu-AB-3PRGD2lutetium Lu 177 AB-3PRGD2
02
Targets
αVβ3 (Integrin αVβ3)
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