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Lecufexor (ID119031166M) is a novel small molecule agonist of the farnesoid X receptor (FXR), developed by Ildong Pharmaceutical. It is a non-steroidal FXR agonist designed to regulate bile acid and lipid metabolism. Activation of FXR in the liver leads to downstream effects such as activation of small heterodimeric partner (SHP), inhibition of CYP7A1 (affecting bile acid synthesis), promotion of bile acid excretion, and inhibition of inflammatory cytokines. In preclinical models for nonalcoholic steatohepatitis (NASH), lecufexor demonstrated efficacy in reducing NAFLD activity and liver fibrosis without significant changes in plasma ALT/AST or LDL-C at effective concentrations. The drug has shown preferential intestinal distribution and does not activate itch receptors like MRGPRX4. Clinical development reached Phase 1 trials for NASH but was terminated in July 2024[5][6][7].
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