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Tropifexor is a highly potent, orally bioavailable, non-bile acid small molecule that acts as a selective agonist of the farnesoid X receptor (FXR), a nuclear receptor involved in regulating bile acid metabolism and signaling. Activation of FXR by tropifexor inhibits bile acid synthesis and increases conjugation, transport, and excretion of bile acids, thereby protecting the liver from harmful effects associated with bile accumulation. Tropifexor was discovered by researchers at Novartis and the Genomics Institute of the Novartis Research Foundation. It has been developed primarily for the treatment of cholestatic liver diseases such as primary biliary cholangitis (PBC) and for nonalcoholic steatohepatitis (NASH). The drug has advanced into phase 2 clinical trials for both NASH and PBC. In preclinical studies, tropifexor demonstrated high potency in upregulating FXR target genes in both liver and intestine tissues[1][3][4][5][6][7][8].
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