YL0010014

YL0010014 is a novel **topoisomerase I inhibitor** used as a cytotoxic payload in multiple antibody-drug conjugates (ADCs), including YL201 (anti-B7H3 ADC), YL202/BNT326 (anti-HER3 ADC), and YL217 (anti-CDH17 ADC). It is linked to monoclonal antibodies via protease-cleavable or enzymatically cleavable linkers, enabling targeted delivery of the cytotoxic payload to tumor cells. The conjugated ADCs have shown promising anti-tumor efficacy in preclinical and phase 1 clinical trials across solid tumors such as small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), esophageal cancer, ovarian cancer, nasopharyngeal cancer (NPC), breast cancer, and colorectal cancer. YL0010014 is released systemically following ADC administration, with serum concentrations peaking approximately 6 hours post-infusion and a mean half-life of about 76–97 hours depending on the dose. Its mechanism of action involves **inhibiting topoisomerase I**, leading to DNA damage and tumor cell apoptosis[1][3][5][7].

Other names

YL0010014YL-0010014YL 0010014