Site specific in-vivo activation of therapeutic drugs

Details Site specific in-vivo activation of therapeutic drugs Site specific in-vivo activation of therapeutic drugs

A - Human Necessities

61

K

167/139, 167/185

A61K 31/715 (2006.01) A61K 38/16 (2006.01) A61K 39/395 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01)

Patent

CA 2025899

SITE SPECIFIC IN-VIVO ACTIVATION OF THERAPEUTIC DRUGS ABSTRACT OF THE DISCLOSURE 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. 36

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