exatecan + triptolide

Exatecan + triptolide is a novel dual-payload antibody-drug conjugate (ADC) platform developed by Chengdu Kanghong Pharmaceutical Group. This platform covalently links two distinct cytotoxic agents—exatecan, a DNA topoisomerase I inhibitor, and triptolide, an RNA polymerase II inhibitor—to the same antibody. The dual-killing mechanism is designed to enhance antitumor efficacy and overcome drug resistance. Specifically, triptolide is released first to downregulate the expression of stress response proteins like heat shock protein 70 (HSP70) and efflux pumps like P-glycoprotein (P-gp), thereby sensitizing tumor cells to the subsequent release of exatecan. Preclinical results in xenograft models have demonstrated significant antitumor activity and a favorable safety profile.

Other names

dual-payload ADC platformEXA + TPL ADC