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PX-102 is a synthetic non-steroidal small molecule that acts as an agonist of the Farnesoid X receptor (FXR), a nuclear bile acid receptor. Developed by Phenex Pharmaceuticals, it was investigated for the treatment of FXR-mediated diseases such as metabolic syndrome and non-alcoholic steatohepatitis (NASH). Activation of FXR by PX-102 regulates bile acid homeostasis and modulates lipid and glucose metabolism in the liver and intestine. Preclinical studies showed that PX-102 reduces intestinal uptake of neutral lipids and cholesterol while enhancing their excretion. It also improves hepatic insulin sensitivity and demonstrates hepatoprotective effects in animal models of liver cirrhosis or fibrosis. Clinical development reached phase I trials in healthy volunteers but was subsequently discontinued[1][2][3][4][5].
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