Drug – bio-affecting and body treating compositions – Enzyme or coenzyme containing – Stabilized enzymes or enzymes complexed with nonenzyme
Patent
1993-10-08
1995-07-18
Stone, Jacqueline
Drug, bio-affecting and body treating compositions
Enzyme or coenzyme containing
Stabilized enzymes or enzymes complexed with nonenzyme
424 9461, 53038815, 514 34, 514 55, 536 20, 536 64, 435177, A61K 3758, A61K 3170, C12N 1106, C07H 15252
Patent
active
054339553
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.
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Bagshawe, Br. J. Cancer (1987), vol. 56 (5), pp. 531-532.
Bagshawe, Br. J. Cancer (1988), vol. 58, pp. 700-703.
Springer et al, Abstract 43 from Thrird International Conference on Monoclonal, Antibody/Immunoconjugates for Cancer, Feb. 4-6, 1988, San Diego, Calif.
Bredehorst Reinhard
Kim Chong-Ho
McCabe Richard
Pomato Nicholas
Vogel Carl-Wilhelm
Akzo N.V.
Blackstone William M.
Gormley Mary E.
Stone Jacqueline
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