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177Lu-DOTA-8-AOC-BBN(7-14)NH2

Development stage: Preclinical
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration: Intravenous

Overview

177Lu-DOTA-8-AOC-BBN(7-14)NH2 is a radiolabeled peptide-based radiotherapeutic designed for targeted radionuclide therapy. It consists of a bombesin (BBN) analogue fragment, specifically BBN(7-14)NH2, which acts as a high-affinity ligand for the gastrin-releasing peptide receptor (GRPr). This peptide is conjugated to the macrocyclic chelator DOTA via an 8-aminooctanoic acid (8-Aoc) hydrocarbon spacer and radiolabeled with the beta-emitting radioisotope Lutetium-177. GRPr is frequently overexpressed in various malignancies, including prostate, breast, and pancreatic cancers. Preclinical studies, particularly in androgen-independent prostate cancer models, have demonstrated its potential to deliver localized radiation to tumor cells, both as a monotherapy and in combination with chemotherapy.

Other names: 177Lu-DOTA-8-Aoc-BBN(7-14)NH2Lutetium-177 DOTA-8-Aoc-BBN(7-14)NH2

Targets

GRPR (Gastrin-releasing peptide receptor)BRS3 (Bombesin receptor subtype 3)NMBR (Neuromedin B receptor)

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