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SW43-DOX is a targeted drug conjugate consisting of the sigma-2 (σ2) receptor agonist SW43 linked to the cytotoxic anticancer agent doxorubicin. The σ2-receptor is a biomarker frequently overexpressed in rapidly proliferating cancer cells, including hepatocellular carcinoma and pancreatic cancer. By leveraging the high affinity of the SW43 ligand for the σ2-receptor, the conjugate facilitates specific tumor cell surface binding and subsequent internalization, delivering the doxorubicin payload directly into the malignant cells. In vitro studies have demonstrated that SW43-DOX exhibits significantly lower EC50 values compared to free doxorubicin across various cancer cell lines, suggesting enhanced antitumoral potency and reduced off-target effects.
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