Zp. Zhu et al., INHIBITION OF EPSTEIN-BARR-VIRUS-TRANSFORMED HUMAN CHRONIC LYMPHOCYTIC LEUKEMIC B-CELLS WITH MONOCLONAL-ANTIBODY ADRIAMYCIN (DOXORUBICIN) CONJUGATES, Cancer immunology and immunotherapy, 40(4), 1995, pp. 257-267
The anthracyclin antineoplastic agent doxorubicin (Adriamycin) was lin
ked by four different methods of linkage to DalB02, an IgG1 kappa muri
ne monoclonal antibody (mAb) against surface-associated antigens on hu
man chronic lymphocytic leukaemia (CLL) B cells. All the four conjugat
es fully retained the immunoreactivity of the parent DalB02. When the
inhibitory effect of these conjugates was evaluated in vitro against t
he target D-10-1, cells (a clone derived from an Epstein-Barr-virus-tr
ansformed human CLL B cell line that binds DalB02) it was observed tha
t one conjugate was more potent than the free drug but the others were
not. When I-131-labelled unmodified DalB02 and the I-131-labelled Dal
B02-containing conjugate that was found to be potent were injected i.v
. into nude mice bearing a subcutaneous D-10-1 xenograft, the percenta
ges of the injected dose (% ID) of both I-131-DalB02 and the I-131-Dal
B02-containing conjugate that localized in the tumour were much higher
than the %ID of the respective preparations that localized in normal
tissues of D-10-1-xenografted mice. The systemic toxicity of the conju
gate was less than that of the free drug. At an equitoxic dose level,
this conjugate was a more effective inhibitor of established D-10-1 xe
nografts than the free drug.