Transferrin was covalently conjugated to adriamycin (Trf-adr) by the f
ormation of a schiff base. This conjugate was found to bind to cell me
mbrane trf receptors in a variety of human tumor cell lines. The Trf-a
dr conjugate was found to be active against sensitive and resistant ce
ll lines e.g. Love, HL-60, H-meso and Hep2. It was, however, found tha
t Trf-adr conjugate was more potent against resistant human tumor cell
lines as compared to sensitive cell lines (based on cytotoxicity assa
ys). The Trf- adr conjugate was then tested against nude mice bearing
human mesothelioma tumors in their peritoneal cavity. The Trf-adr conj
ugate prolonged the lifespan of advanced tumor bearing nude mice as co
mpared to either adriamycin alone or adriamycin and trf unlinked. Our
studies show that trf call be succesfully used as an ligand for direct
ing anticancer drugs to human tumor cells.