Drug intelligence / Profile preview

Lumi804-trastuzumab

Development stage
Preclinical
Lead developer
Washington University School of Medicine
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Lumi804-trastuzumab (also known as Lumi804-Tz) is a preclinical theranostic radioimmunoconjugate consisting of the human epidermal growth factor receptor 2 (HER2)-targeting monoclonal antibody trastuzumab conjugated to Lumi804, a proprietary octadentate macrocyclic chelator based on four 1-hydroxypyridin-2-one (1,2-HOPO) coordinating units developed by Lumiphore. The conjugate is designed to stably chelate various radiometals, enabling both diagnostic imaging and targeted radionuclide therapy. Specifically, it can be radiolabeled with zirconium-89 (89Zr) for positron emission tomography (PET) imaging or with thorium-227 (227Th) for targeted alpha therapy. In preclinical models of colorectal cancer, the 227Th-labeled conjugate demonstrated significant tumor growth inhibition and extended survival, while the 89Zr-labeled counterpart served as an effective imaging partner, confirming its potential as a theranostic pair.

Other names
227Th-Lumi804-trastuzumab89Zr-Lumi804-trastuzumabLumi804-TzLumi-804-TzLumi 804-Tz
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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