OA-235i

OA-235i is a synthetic, cell-penetrating, lipidated peptide developed using Pepducin technology to act as a potent and specific antagonist of protease-activated receptor 2 (PAR2), a G-protein coupled receptor implicated in inflammation and fibrosis. By blocking PAR2 signaling in hepatic stellate cells, inflammatory cells, and hepatocytes, OA-235i demonstrates anti-fibrotic and anti-inflammatory effects. Preclinical studies have shown that it significantly reduces liver steatosis, inflammation, ballooning injury (NAS score), ALT levels by 50%, and completely suppresses AST in mouse models of diet-induced nonalcoholic steatohepatitis (NASH). It also suppresses weight gain, liver weight, triglycerides, steatosis progression, development of liver tumor foci in long-term NASH models, and severe fibrosis induced by CCl4 exposure. The drug has shown safety with no organ toxicity at high multiples of the therapeutic dose in animal studies. Clinical development is ongoing for nonalcoholic fatty liver disease (NAFLD), NASH, alcoholic hepatitis/fatty liver disease; additional preclinical work targets hepatocellular carcinoma (HCC), pain syndromes related to PAR2 activation pathways such as inflammatory bowel diseases and fibrosis[1][2][6].

Other names

PAR2 inhibitor pepducinsPAR-2 inhibitor pepducinsPAR 2 inhibitor pepducins