Enzyme-cleavable prodrug compounds

US7425541B2 · kind B2 · utility

Assignee

• MEDAREX INC. · US

Inventors

• Vincent Dubois · Ittre, BE
• Ann Marie Fernandez · Brussels, BE
• Sanjeev Gangwar · Foster City, US
• Evan Lewis · Pacifica, US
• Thomas J. Lobl · Valencia, US
• Matthew H. Nieder · Seattle, US
• Lesley Pickford · Menlo Park, US
• Andre Trouet · Winksele, BE
• Geoffrey T. Yarranton · Burlingame, US

Key dates

• Filing date: Jun 11, 2001
• Grant date: Sep 16, 2008
• Expiry date: May 15, 2023

Classification

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

Abstract

The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.