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177Lu-TATE-RGD
- Development stage
- Phase 1
- Lead developer
- Peking Union Medical College Hospital
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
177Lu-TATE-RGD is a novel dual-targeted therapeutic radiopharmaceutical developed for the treatment of tumors expressing both somatostatin receptor subtype 2 (SSTR2) and integrin αVβ3. It consists of a peptide conjugate that combines a somatostatin analog (TATE, typically targeting SSTR2) with an RGD motif (targeting integrin αVβ3), labeled with the beta-emitting radionuclide lutetium-177. This design enables simultaneous targeting of neuroendocrine tumor cells and tumor vasculature, potentially improving efficacy over single-target agents. The drug is being developed primarily for neuroendocrine tumors and adenomatous polyposis coli, with early clinical trials underway in China. Its mechanism involves binding to SSTR2 and integrin αVβ3 on tumor cells or neovasculature, followed by internalization and delivery of cytotoxic radiation from lutetium-177 to induce cell death[1][4][10].
- Brand names
- 177Lu-TATE-RGD
02
Targets
αVβ3 (Integrin αVβ3)SSTR2 (Somatostatin receptor type 2)
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