ZW-251 is a glypican-3 ( GPC3 )-targeted antibody-drug conjugate ( ADC ) with topoisomerase-I inhibitory activity. ZW-251 induces cytotoxicity, penetrates tumor spheroids, exerts bystander cytotoxicity, and inhibits tumor growth in hepatocellular carcinoma models. ZW-251 can be used for the research of hepatocellular carcinoma [1] [2].
In Vivo, ZW-251 (20-120 mg/kg; i.v.; 3 doses at day 1, 22 and 43) is well tolerated in cynomolgus monkeys and exhibits dose-proportional PK[2].
In Vitro, ZW-251 (0.001-100 nM; 4 days) exhibits cell cytotoxicity to HepG2 spheroid liver cancer cell line[2].
References:
[1]. Chandana, et al. A phase 1, first-in-human, multicenter study of ZW251, a novel glypican-3 (GPC3)–targeted antibody-drug conjugate (ADC), in participants with hepatocellular carcinoma (HCC). J Clin Oncol. 2026 Jan 12;44(Number 2_Suppl):TPS608.
[2]. Madera L, et al. ZW251, a novel glypican-3-targeting antibody-drug conjugate bearing a topoisomerase I inhibitor payload, demonstrates compelling preclinical activity in hepatocellular carcinoma models. 2024.
In Vivo, ZW-251 (20-120 mg/kg; i.v.; 3 doses at day 1, 22 and 43) is well tolerated in cynomolgus monkeys and exhibits dose-proportional PK[2].
In Vitro, ZW-251 (0.001-100 nM; 4 days) exhibits cell cytotoxicity to HepG2 spheroid liver cancer cell line[2].
References:
[1]. Chandana, et al. A phase 1, first-in-human, multicenter study of ZW251, a novel glypican-3 (GPC3)–targeted antibody-drug conjugate (ADC), in participants with hepatocellular carcinoma (HCC). J Clin Oncol. 2026 Jan 12;44(Number 2_Suppl):TPS608.
[2]. Madera L, et al. ZW251, a novel glypican-3-targeting antibody-drug conjugate bearing a topoisomerase I inhibitor payload, demonstrates compelling preclinical activity in hepatocellular carcinoma models. 2024.