Definition

A peptide-drug conjugate (PDC) composed of a peptide conjugated, via an aminopeptidase-targeting linkage, to an as of yet undisclosed alkylating agent, with potential antineoplastic activity. Upon administration, PDC OPD5 is hydrolyzed by peptidases to release the alkylating agent, thereby allowing for specific accumulation of the agent in aminopeptidase-positive tumor cells. This may result in the inhibition of DNA and/or RNA synthesis and the induction of apoptosis, thereby inhibiting tumor cell proliferation. Peptidases are overexpressed by certain cancer cells.