초록

Prodrugs that are activated by and conjugated to a catalytic antibody conjugated to a moiety that binds to a tumor cell population are provided.

대표청구항 ▼

[ What is claimed is:] [1.]1. A prodrug of the formula P-X, wherein X is a radical of a drug XOH and P is a protecting group of the formulaR.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or not the same and are selected from the group consisting of H, alkyl with 1-10 carbon atoms, alkoxy

[ What is claimed is:] [1.]1. A prodrug of the formula P-X, wherein X is a radical of a drug XOH and P is a protecting group of the formulaR.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or not the same and are selected from the group consisting of H, alkyl with 1-10 carbon atoms, alkoxy with 1-10 carbon atoms, monocyclic aromatic, alkene with 1-10 carbon atoms, hydroxyl, hydroxyalkyl, amino alkyl, thioalkyl, amino, alkylamino, alkylphosphonate, alkylsulfonate, alkylcarboxylate, and alkylammonium, with the proviso that at least one of R.sup.1-5 is not H and said prodrug is not Ara-C-2,4,6-trimethyl benzoate, Ara-C-3,4,5-trimethoxy benzoate, Ara-C-p-methoxy benzoate or Ara-C-2,6-dimethyl benzoate,wherein said prodrug is activated by and conjugated to a catalytic antibody conjugated to a moiety capable of binding to a specific cell population, wherein the moiety is selected from the group consisting of a tumor-selective antibody, a binding protein of a tumor-associated protein, and a tumor-selective receptor ligand, said catalytic antibody enhances the rate of cleavage of said protective group on said prodrug, and said prodrug is stable to endogenous mammalian enzymes.