oxyphenisatin acetate

Oxyphenisatin acetate is a small molecule pro-drug of oxyphenisatin (3,3-bis(4-hydroxyphenyl)-1H-indol-2-one) that was formerly used as a stimulant laxative. It was introduced in the US as Lavema by Winthrop in 1959 and marketed under several brand names. Oxyphenisatin acetate acts primarily by stimulating bowel movements and was used both orally and as an enema for constipation and preoperative bowel preparation[7][5]. Long-term use is associated with liver toxicity, including jaundice and liver damage; these safety concerns led to its withdrawal from most markets in the early 1970s[2][5][7]. Mechanistically, recent studies have shown that it can inhibit cancer cell growth by inducing a multifaceted cell starvation response involving inhibition of protein synthesis (via phosphorylation of eIF2α kinases GCN2 and PERK), activation of AMP-activated protein kinase (AMPK), reduced mTOR signaling, autophagy induction, mitochondrial dysfunction, ATP depletion, TNFα signaling modulation, and oncosis—a form of nonapoptotic cell death[6][8]. Its primary historical indication was for constipation.

Brand names

AcetalaxContaxIsocrin

Other names

oxyphenisatin acetateacetophenolisatin