M-COPA

M-COPA (formerly known as AMF-26) is an orally active, small-molecule Golgi disruptor that targets the activation of ADP-ribosylation factor 1 (Arf1). It was developed by Eisai in collaboration with the Japanese Foundation for Cancer Research and Tokyo University of Science. M-COPA acts by binding to the contact surface of the Arf1-Sec7 domain, thereby inhibiting the interaction between Arf1 and its guanine nucleotide exchange factor (GEF). This blockade prevents Arf1 activation, leading to the disruption of the Golgi apparatus, inhibition of biosynthetic protein trafficking (such as receptor tyrosine kinases like MET, EGFR, and Kit to the cell surface), and induction of apoptosis. M-COPA has demonstrated potent preclinical antitumor activity in various cancer models, including breast, gastric, and non-small cell lung cancers, particularly those with receptor tyrosine kinase alterations or resistance to tyrosine kinase inhibitors.

Other names

(2E,4E)-5-((1S,2S,4aR,6R,7S,8S,8aS)-7-hydroxy-2,6,8-trimethyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl)-2-methyl-N-(pyridin-3-ylmethyl)penta-2,4-dienamide2-methylcoprophilinamidemethylcoprophilinamide