Drug intelligence / Profile preview

[225Ac]hu11B6-IgG3R435H

Development stage
Preclinical
Lead developer
Diaprost
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[225Ac]hu11B6-IgG3R435H is a preclinical-stage targeted alpha-particle radioimmunotherapy (TAT) agent developed by DiaProst AB. It consists of a humanized monoclonal antibody, hu11B6, engineered into an IgG3 subclass with an R435H Fc mutation designed to enhance binding to the neonatal Fc receptor (FcRn) and optimize its pharmacokinetic profile. The antibody is conjugated via a DOTA chelator to the alpha-emitting radionuclide Actinium-225 (225Ac). It specifically targets human kallikrein 2 (hK2/KLK2), a serine protease that is highly and almost exclusively expressed in prostate tissue and prostate cancer cells, including those in castration-resistant and androgen receptor-addicted states. Upon binding and internalization, the alpha radiation delivers high-energy particles that induce lethal double-strand DNA breaks in the tumor cells while minimizing damage to surrounding healthy tissue.

Other names
Actinium-225-labeled hu11B6-IgG3R435HActinium225-labeled hu11B6-IgG3R435HActinium 225-labeled hu11B6-IgG3R435H225Ac-hu11B6-IgG3R435H
02

Targets

HK2 (Hexokinase Type II)

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