Immunoconjugates and prodrugs and their use in association for drug delivery.

摘要

A drug delivery system is described in which an immunoconjugate and a prodrug are used in association with each other to deliver a drug to a host target site such as a tumour. The immunoconjugate comprises an antibody or antibody fragment to which is attached a beta -lactamase or an active fragment thereof. The prodrug is a cyclic amide derivative of a drug or an unstable precursor thereof in which the drug or precusor is attached to the remainder of the prodrug such that it forms a leaving group which on hydrolysis of the prodrug is eliminated as the active drug or unstable precursor. Particular prodrugs include penicillin or cephalasporin derivatives and other beta -lactams to which are attached any physiologically active substances, particularly antineoplastic agents, antiviral, antibacterial or antifungal compounds. In use the immunoconjugate is adminstered first such that it localises at the host target site. Subsequent administration of the prodrug results in beta -lactamase catalysed hydrolysis of the prodrug at the target site with release of the active drug or unstable precursor.