USE OF INTRACELLULAR ENZYMES FOR THE RELEASE OF COVALENTLY LINKED BIOACTIVES

摘要

The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.

主权项

1. A method of using an intracellular enzyme to increase the efficaciousness of a linked bioactive in a specific target tissue for the treatment of a disease in a patient in need thereof, wherein the linked bioactive upon cleavage by the intracellular enzyme displays a synergistic effect between the two bioactives which is not observed when the bioactives are administered alone or in non-linked bioactives.