Oxyphenisatin

Oxyphenisatin is a synthetic small molecule stimulant laxative belonging to the indole class. It was introduced in the United States as Lavema by Winthrop in 1959 and used both orally and as an enema for the treatment of constipation, preoperative bowel preparation, and radiological procedures involving the gastrointestinal tract[4][7]. Oxyphenisatin acts primarily by stimulating peristalsis in the colon through direct action on intestinal mucosa. The drug undergoes enterohepatic circulation. Long-term use has been associated with hepatotoxicity (notably jaundice and liver damage), leading to its withdrawal from most markets in the early 1970s[2][4][7]. Its acetate derivative (oxyphenisatin acetate) is a pro-drug that has also shown antiproliferative activity against certain cancer cell lines via mechanisms involving inhibition of protein synthesis, activation of eIF2α kinases (GCN2 and PERK), AMPK activation, mTOR pathway inhibition, autophagy induction, mitochondrial dysfunction, and TNFα-mediated apoptosis[5][6].

Brand names

Lavema

Other names

oxyphenisatine3,3-bis(4-hydroxyphenyl)-1H-indol-2-one