Targeted alpha particle therapy using actinium-255 conjugates

US6683162B2 · kind B2 · utility

Assignee

• Sloan Kettering Institute for Cancer Research · US

Inventors

• David A. Scheinberg · New York, US
• Dangshe Ma · Millwood, US
• Michael R. McDevitt · New York, US
• Paul Borchardt · New York, US

Key dates

• Filing date: Sep 14, 2001
• Grant date: Jan 27, 2004
• Expiry date: Sep 14, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides functionalized chelants and a method of treating cancerous cells with alpha particles comprising the step of administering a pharmacologically effective dose of an 225Ac conjugate comprising a functionalized chelant R is independently CHQCO2X; Q is independently hydrogen; C1-C4 alkyl or (C1-C2 alkyl) phenyl; X is independently hydrogen; benzyl or C1-C4 alkyl; Z1 is (CH2)nY where n is 1-10 and Y is an electrophilic or nucleophilic moiety and Z2 is R; or, alternatively, Z1 is hydrogen and Z2 is a peptide linker composed of 1-10 amino acids; said Y or said peptide linker covalently attached to an antibody or fragment thereof, or other biologic molecule; or a pharmaceutically acceptable salt thereof, complexed with 225Ac. These biologic molecule binds to cancerous cells and 225Ac or its daughters emit alpha particles into said cancerous cells effecting treatment.