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

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.

REFERENCES:
patent: 4067774 (1978-01-01), Rubenstein
patent: 4804750 (1989-02-01), Nishimura et al.
patent: 4975278 (1990-12-01), Senter et al.
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.

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