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161Tb-DOTA-LM3

Development stage
Phase 1
Lead developer
Paul Scherrer Institute
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

161Tb-DOTA-LM3 is a peptide conjugate radiopharmaceutical designed for targeted therapy of neuroendocrine tumors. It consists of the somatostatin receptor subtype 2 (SSTR2) antagonist DOTA-LM3 labeled with the radionuclide terbium-161 (161Tb). The drug delivers cytotoxic radiation to tumor cells by binding to SSTR2, which is overexpressed in many neuroendocrine neoplasms. Unlike traditional SSTR2 agonist-based therapies, DOTA-LM3 as an antagonist binds to more receptor sites and accumulates mainly on the cell membrane. The attached terbium-161 emits both beta particles and a high number of Auger electrons upon decay; these Auger electrons deposit their energy over extremely short distances, resulting in highly localized damage that increases tumor cell kill while sparing surrounding healthy tissue. Preclinical studies have shown that 161Tb-labeled compounds are significantly more effective than their lutetium-177 counterparts at inhibiting tumor viability and delivering higher local doses to cancer cells[1][2][4][5]. The drug is currently being evaluated in early-phase clinical trials for gastroenteropancreatic neuroendocrine tumors.

Other names
Terbium-161-DOTA-LM3Terbium161-DOTA-LM3Terbium 161-DOTA-LM3
02

Targets

SSTR2 (Somatostatin receptor type 2)

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