ACXT-3102

ACXT-3102 (also known as Sigma-2-Erastin or S2E) is an orally bioavailable small molecule conjugate designed to treat pancreatic cancer by inducing both apoptosis and ferroptosis. Developed by Accuronix Therapeutics, the compound consists of a sigma-2 receptor ligand linked to dm-Erastin, an inhibitor of the cystine/glutamate antiporter (xCT). The sigma-2 ligand serves as a cancer-targeted delivery moiety, as sigma-2 receptors are highly overexpressed in various solid tumors, including pancreatic cancer. Upon binding and internalization, ACXT-3102 inhibits xCT, leading to glutathione depletion, decreased GPX4 expression, and the accumulation of lipid reactive oxygen species (ROS). This triggers cell death through the lipid ROS-DUSP6-MAPK/ERK signaling pathway. Preclinical data from murine xenograft models have shown that ACXT-3102 significantly reduces tumor volume and improves survival.

Other names

Sigma-2-ErastinSigma2-ErastinSigma 2-Erastin