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Garetatug rezetecan is an investigational antibody-drug conjugate targeting claudin 18.2, a tight junction protein overexpressed in subsets of gastric and gastroesophageal junction adenocarcinomas. It consists of the humanized monoclonal antibody garetatug directed against claudin 18.2 conjugated via a cleavable linker to the topoisomerase I inhibitor payload rezetecan, enabling selective delivery of a cytotoxic agent to claudin 18.2–positive tumor cells and induction of DNA damage–mediated cell death.[9][12] Developed by Shanghai Hengrui Pharmaceutical/Jiangsu Hengrui Medicine, the drug has shown a manageable safety profile and encouraging objective response rates in early-phase trials of patients with advanced claudin 18.2–positive gastric or gastroesophageal junction cancer and is being further evaluated in phase II and III studies in this setting.[1][2][3][9]
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