211-astatine containing radiotherapeutics for the treatment of cancer

US10457642B2 · kind B2 · utility

Assignee

• The Trustees of the University of Pennsylvania · US

Inventors

• Daniel A. Pryma · Via Enrico Fermi, US
• Brian LIEBERMAN · Philadelphia, US
• Mehran Makvandi · Philadelphia, US
• Robert H. Mach · Eureka, US

Key dates

• Filing date: Apr 26, 2016
• Grant date: Oct 29, 2019
• Expiry date: Apr 26, 2036

Classification

• Technology area (CPC G): Physics
• CPC primary: G21H5/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.