Hemay181

Hemay181 is a novel sugar-linked drug conjugate (SDC) designed as a broad-spectrum cytotoxic agent for the treatment of advanced solid tumors. It functions by releasing the cytotoxic payload SN-38 within tumor tissues through metabolism by β-glucuronidase, an enzyme highly expressed in hypoxic tumor microenvironments but with low activity in normal tissues. The released SN-38 inhibits topoisomerase I, thereby blocking DNA replication and inducing cell death in cancer cells. Hemay181 demonstrates significantly improved water solubility compared to SN-38 and binds plasma albumin to form a macromolecular transporter, enhancing pharmacokinetics and tumor selectivity. Preclinical studies have shown efficacy across multiple human tumor cell lines and xenograft models, including colorectal, gastric, triple-negative breast, head and neck, pancreatic, lung, prostate cancers, and melanoma[1]. As of 2024–2025 it is undergoing Phase 1 clinical trials for advanced solid tumors[2][3][4][6].