Animal experiment:

Assessment in several other tumor models demonstrates tolerability with oxyphenisatin acetate at 300 mg/kg given once daily or 200 mg/kg given twice daily. For the MCF-7 study treatments are administered on an exact body weight basis using dose volumes of 1-2 mL/kg body weight. The vehicle control receives 100% DMSO. The treated group receives 300 mg/kg oxyphenisatin acetate once daily for a total of 10 days, followed by a 3 day rest and an additional 6 days of dosing. The dose solutions are prepared in 100% DMSO, aliquoted and stored frozen until used. The mice are monitored for a total of 52 days with treatment initiation occurring on day 27 posttumor implantation[1].

Oxyphenisatin acetate, the pro-drug of oxyphenisatin, is used to be a laxative.

Oxyphenisatin acetate inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T, and MDA-MB-468. In the estrogen receptor (ER) positive MCF7 and T47D cells, oxyphenisatin acetate induces TNFα expression and TNFR1 degradation, indicating autocrine receptor-mediated apoptosis in these lines. Ten micromoles per liter Oxyphenisatin acetate treatment results in autophagy and mitochondrial dysfunction[1].

Oxyphenisatin acetate (300 mg/kg, i.p.) delivers intraperitoneally inhibited tumor growth, accompanied by phosphorylation of eIF2α and degradation of TNFR1 in an MCF7 xenograft model[1].

[1]. Morrison BL, et al. Oxyphenisatin acetate (NSC 59687) triggers a cell starvation response leading to autophagy, mitochondrial dysfunction, and autocrine TNFα-mediated apoptosis. Cancer Med. 2013 Oct;2(5):687-700.