YH012 is a novel bispecific HER2/TROP2 antibody-drug conjugate (BsAb-ADC) developed using the RenLiteTM platform. The TAAs HER2 and TROP2 are highly co-expressed in a variety of solid tumors, implying multiple potential indications for YH012. Bispecificity of YH012 enhances selective endocytic uptake of BsAbs into HER2/TROP2 co-expressing tumor cells resulting in enrichment of anti-mitotic payload (MMAE) delivery and enhanced anti-tumor efficacy compared to controls. The backbone of YH012 was constructed using RenLiteTM mice and the preexisting “knobs-into-holes” (KiH) heterodimerization method, demonstrating the value of this workflow to for rapidly generating BsAb-ADCs of unequaled purity, stability, and functional potential.