Medarex Inc.

Coulter Pharmaceutical, Inc.

Vincent Dubois

Andre Trouet

Sanjeev Gangwar

Geoffrey T Yarranton

Thomas Jay Lobl

Lesley B Pickford

Matthew H Nieder

Christopher Robert Bebbington

Ann Marie Fernandez

Evan Lewis

Alexandre Passioukov

André Trouet

Thomas J Lobl

Peter Viski

Anne-Marie Fernandez

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.

Enzyme-cleavable prodrug compounds

The product of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide having a plasmin peptide substrate of 2-4 amino acids and mono- or di-peptide linkage, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by plasmin. Also disclosed are methods of making and using the prodrug compounds.

Prodrugs activated by plasmin and their use in cancer chemotherapy

The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.

Tripeptide prodrug compounds

Growing community of inventors

Fleurus, Belgium

Vincent Dubois