Methods for tumor diagnosis and therapy

摘要

The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.

主权项

1. A method for delivering a radiation dose to a tissue in a subject, the method comprising:
(i) administering to a subject in need thereof an effective amount of a water-soluble prodrug molecule, wherein said prodrug is represented by the formula:wherein
R1 is selected from the group consisting of a hydrogen radical, a radionuclide, a molecule labeled with one or more radionuclides, a boron atom, a moiety labeled with one or more boron atoms, and a boron cage; R2 is selected from the group consisting of a hydrogen radical, a radionuclide, and a boron cage; at least one of R1 and R2 is not a hydrogen radical; and R3 is a prosthetic group that can be cleaved by an enzyme; said prodrug being a substrate for the enzyme and hydrolyzed by said enzyme molecules present within the tissue, said hydrolysis forming a water-insoluble drug precipitate, and (ii) if R1 or R2 comprises at least one boron atom, activating the boron atom with epithermal neutrons; such that a radiation dose is delivered to the tumor.