Drug intelligence / Profile preview

[77Br]Br-WC-DZ

Development stage
Preclinical
Lead developer
Washington University in St. Louis
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[77Br]Br-WC-DZ is a PARP-1 targeted radiopharmaceutical designed for the treatment of advanced prostate cancer. It consists of a PARP-1 inhibitor (WC-DZ) labeled with the Auger-emitting radionuclide Bromine-77 (77Br). Because PARP-1 is a chromatin-binding enzyme overexpressed in prostate cancer and located in close proximity to cellular DNA, the drug delivers high-linear energy transfer (LET) Auger radiation directly to the genome. This localized radiation induces lethal double-strand DNA breaks, G2-M cell cycle arrest, and cytotoxicity. Preclinical studies in prostate cancer xenograft models have demonstrated its ability to inhibit tumor growth and improve survival.

Other names
77Br-labeled PARP-1 inhibitorradio-brominated Auger emitting PARP inhibitor
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)

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