Mocertatug rezetecan (DAR4) (HS-20089 (DAR4); GSK5733584 (DAR4)) is an antibody-drug conjugate ( ADC ) targeting B7-H4, composed of Mocertatug and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan. Mocertatug rezetecan (DAR4) delivers a TOPO1 inhibitor payload. It binds to B7-H4 -expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan (DAR4) exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer [1] [2] [3].
In Vivo, Mocertatug rezetecan (DAR4) exhibits significant and dose-dependent tumor growth inhibition in MX-1 (breast cancer) and RL95-2 (endometrial cancer) CDX models[3].
In Vitro, Mocertatug rezetecan (DAR4) binds concentration-dependently to B7-H4-expressing tumor cells, drives time-dependent B7-H4 internalization and cellular cytotoxicity, induces S-phase cell cycle arrest, and exhibits bystander killing capability[3].
References:
[1]. Zhou L, et al. The role of B7-H4 in ovarian cancer immunotherapy: current status, challenges, and perspectives. Frontiers in immunology. 2024;15:1426050.
[2]. Wu J, et al. 381O First-in-human/phase I trial of HS-20089, a B7-H4 ADC, in patients with advanced solid tumors[J]. Annals of Oncology, 2023, 34: S336.
[3]. Waight J, et al. Non-clinical characterization of Mocertatug Rezetecan (GSK5733584), a novel B7-H4-directed antibody-drug conjugate[J]. Cancer Research, 2026, 86(7_Supplement): 4575-4575.
In Vivo, Mocertatug rezetecan (DAR4) exhibits significant and dose-dependent tumor growth inhibition in MX-1 (breast cancer) and RL95-2 (endometrial cancer) CDX models[3].
In Vitro, Mocertatug rezetecan (DAR4) binds concentration-dependently to B7-H4-expressing tumor cells, drives time-dependent B7-H4 internalization and cellular cytotoxicity, induces S-phase cell cycle arrest, and exhibits bystander killing capability[3].
References:
[1]. Zhou L, et al. The role of B7-H4 in ovarian cancer immunotherapy: current status, challenges, and perspectives. Frontiers in immunology. 2024;15:1426050.
[2]. Wu J, et al. 381O First-in-human/phase I trial of HS-20089, a B7-H4 ADC, in patients with advanced solid tumors[J]. Annals of Oncology, 2023, 34: S336.
[3]. Waight J, et al. Non-clinical characterization of Mocertatug Rezetecan (GSK5733584), a novel B7-H4-directed antibody-drug conjugate[J]. Cancer Research, 2026, 86(7_Supplement): 4575-4575.