Synthesis, characterization and targeting chemotherapy for ovarian cancer of trastuzumab-SN-38 conjugates

Schematic displays the structures of three HER2-targeting antibody-drug conjugates (ADCs): T-SN38 A, T-SN38 B and T-SN38 C. T-SN38 A prepared with the hydrophobic ester linkage linker A which contained ester bond cleavage site; T-SN38 B contains hydrophobic linker B with carbonate cleavage site; T-SN38 C contains linker C with hydrophilic PEG4 fragment and carbonate cleavage site. Results of in vitro and in vivo showed T-SN38 A, B and C (Drug Antibody Rate, DAR = 3.7, 3.2, 3.4) have great potential for HER2-positive ovarian cancer.171