Richard Lawrence Mccabe

US Patent:

54339553, Jul 18, 1995

Filed:

Oct 8, 1993

Appl. No.:

8/134520

Inventors:

Reinhard Bredehorst - Washington DC
Chong-Ho Kim - Rockville MD
Richard McCabe - Rockville MD
Nicholas Pomato - Frederick MD
Carl-Wilhelm Vogel - Washington DC

Assignee:

Akzo N.V. - Arnhem

International Classification:

A61K 3758
A61K 3170
C12N 1106
C07H 15252

US Classification:

424 943

Abstract:

A method for site-specific in-vivo activation of a prodrug in an animal using an activator-targeting moiety conjugate to localize an activator at a predetermined site of use and a prodrug compound that is converted to an active drug in the presence of the activator. In the preferred embodiment, the targeting moiety, the activator, and the prodrug demonstrate little or no immunogenicity in the animal being treated. The targeting moiety is relatively specific for binding to the target tissue than to non-target tissue. The activator is not found or present in only small amounts in circulation or in non-target tissue, does not have a substrate for its activity in circulation or in non-target tissue, can be linked to the targeting moiety, and is capable of converting the prodrug to an active drug. The prodrug is selected for its ability to exert a cytotoxic activity on the target tissue after conversion by the activator.