Drug intelligence / Profile preview

99mTc-AO-BBN

Development stage
Preclinical
Lead developer
Universidade de Lisboa
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

99mTc-AO-BBN is a dual-targeted radiopharmaceutical conjugate designed for targeted radionuclide therapy and imaging, specifically investigated in the context of prostate cancer. The molecule consists of a technetium-99m (99mTc) radionuclide complexed with a bombesin (BBN) derivative and an acridine orange (AO) moiety. The bombesin component targets the gastrin-releasing peptide receptor (GRPR), which is frequently overexpressed on the surface of various cancer cells, including human prostate cancer PC3 cells. The acridine orange component serves as a nuclear localizing agent by intercalating into DNA. This dual-targeting strategy aims to internalize the radioconjugate and transport it to the nucleus, where the short-range Auger electrons emitted by 99mTc can effectively induce DNA damage, such as double-strand breaks (evidenced by γH2AX foci) and micronuclei formation, leading to enhanced cell death compared to single-targeted analogs.

Other names
99mTc-labeled acridine orange-bombesin conjugate
02

Targets

GRPR (Gastrin-releasing peptide receptor)

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