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Turofexorate isopropyl is a potent, selective, and orally bioavailable small molecule agonist of the farnesoid X receptor (FXR), also known as the bile acid receptor. It was originally discovered by Exelixis and later licensed to Wyeth, which became a subsidiary of Pfizer. The drug binds to the ligand-binding domain of human FXR and promotes transcription of genes involved in bile acid metabolism such as BSEP, SHP, and IBABP. Turofexorate isopropyl has demonstrated activity in suppressing lipid peroxidation and inhibiting ferroptotic cell death through FXR activation. It was investigated for metabolic diseases including hyperlipidemia, atherosclerosis, and nonalcoholic steatohepatitis (NASH), but development has been discontinued at phase 1[2][3][4][5][6].
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