In vitro efficacy of DM001:
DM001 showed high affinity and cytotoxicity in multiple TROP2+ EGFR+ cancer cell lines. DM001 delayed cell cycle progression and induced apoptosis in cancer cells. DM001 bsADC showed preferential binding to cells expressing both TROP2 and EGFR, indicating potentially better safety in single positive cells.
DM001 exhibited potent and dose-dependent anti-tumor efficacy in multiple CDX and PDX models. DM001 showed stronger efficacy than benchmarks Sacituzumab govitecan, Cetuximab and MGR003-analog. While the efficacy of DM001 was higher than its parental ADCs in PDX models, it was not obvious in CDX models, indicating that DM001 may be more effective in targeting heterogeneous tumors, which better mimics the tumor microenvironment in patients.