BIFUNCTIONAL GLYCOPROTEINS HAVING A MODIFIED CARBOHYDRATE COMPLEMENT, AND THEIR USE IN TUMOR-SELECTIVE THERAPY

摘要

Provided herein are carbohydrate complement-modified bifunctional glycoproteins, and their use in tumorselective therapy. The bifunctional glycoproteins comprise a first component that specifically binds to a tumor-specific antigen and a second component having enzymic activity by means of which a non-toxic prodrug is cleaved into a cytotoxic drug. The carbohydrate complement comprises at least one exposed carbohydrate residue selected from the group consisting of mannose, galactose, N-acetylglucosamine, lactose and fucose. The modified carbohydrate complement contributes to increased relative concentration of the glycoproteins at the site of the tumor, and enhanced clearance from the general circulation and non-tumor sites.