Medarex Inc.

Coulter Pharmaceutical, Inc.

Matthew H Nieder

Sanjeev Gangwar

Lesley B Pickford

Geoffrey T Yarranton

Thomas Jay Lobl

Christopher Robert Bebbington

Andre Trouet

Vincent Dubois

Chin Pan

André Trouet

Pina M Cardarelli

Evan Lewis

Ann Marie Fernandez

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 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

The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the CD10 enzyme. Methods of treatment using the prodrug and methods of designing the prodrug are also disclosed.

CD10-activated prodrug compounds

The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.

Prodrug compounds with isoleucine

The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the CD10 enzyme. Methods of treatment using the prodrug and methods of designing a prodrug are also disclosed.

CD-10 activated prodrug compounds

Prodrug compounds with an isoleucine

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Burlingame, CA, United States of America

Matthew H Nieder