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actinium-225 nectin-4-targeted radiopharmaceutical therapy

Development stage
Preclinical
Lead developer
Aptevo Therapeutics
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Aptevo Research's Nectin-4-targeted radiopharmaceutical therapy is a preclinical-stage therapeutic candidate developed in collaboration with NioWave. The asset utilizes a targeting moiety specific to Nectin-4 (Poliovirus receptor-related protein 4) to deliver the alpha-emitting radioisotope Actinium-225 (Ac-225) directly to tumor cells. Nectin-4 is a cell adhesion molecule that is significantly overexpressed in various solid malignancies, including urothelial, breast, and lung cancers, making it a viable target for selective delivery of cytotoxic payloads. The mechanism of action involves the binding of the radiopharmaceutical to Nectin-4 on the surface of cancer cells, followed by the emission of high-energy alpha particles from the Ac-225 isotope. These alpha particles cause complex, difficult-to-repair double-strand DNA breaks within the target cells, leading to cell death while minimizing exposure to adjacent healthy tissues due to the short range of alpha radiation.

Other names
ac-225ac225ac 225actinium-225actinium225actinium 225Actinium-225 Nectin-4 RPTActinium225 Nectin-4 RPTActinium 225 Nectin-4 RPT
02

Targets

PVRL4 (Nectin cell adhesion molecule 4)

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