anti-TROP2 parental antibody-drug conjugate

The anti-TROP2 parental antibody-drug conjugate is a monovalent therapeutic agent designed to target Trophoblast cell-surface antigen 2 (TROP2), a glycoprotein overexpressed in various epithelial tumors, including urothelial carcinoma. Developed by Biocytogen using their RenLite® transgenic mouse platform, this ADC serves as a monovalent precursor and benchmark for the development of bispecific ADCs, such as BCG039 (a Nectin-4 x TROP2 bispecific ADC). The parental ADC has been evaluated using two distinct linker-payload systems: the microtubule inhibitor monomethyl auristatin E (MMAE) conjugated via a valine-citrulline (vc) linker, and Biocytogen’s proprietary BLD1102 platform, which utilizes a novel Topoisomerase I (TOP1) inhibitor payload and a highly hydrophilic, enzyme-cleavable linker. In preclinical studies, the parental ADC demonstrated anti-tumor activity in CDX and PDX models, although it typically exhibits lower potency and internalization kinetics compared to its bispecific derivatives, which benefit from cooperative binding between two distinct tumor-associated antigens.

Other names

monovalent TROP2 ADCTROP2-targeting parental ADCTROP-2-targeting parental ADCTROP 2-targeting parental ADCanti-TROP2 monovalent ADCanti-TROP-2 monovalent ADCanti-TROP 2 monovalent ADC