Drug intelligence / Profile preview

SW43-DOX

Development stage
Preclinical
Lead developer
Yale University
Modality
Small Molecules
Administration
Intravenous, Intra-arterial
01

Overview

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.

Other names
SW43-doxorubicin conjugateSW-43-doxorubicin conjugateSW 43-doxorubicin conjugate
02

Targets

TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))SIGMAR1 (Sigma non-opioid intracellular receptor 1)TOP2A (DNA topoisomerase II)

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