IDG16177 / Evotec, Ildong 
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  • ||||||||||  IDG16177 / Evotec, Ildong
    In Vitro DILI Risk Assessment of IDG16177, a Potent and Selective GPR40 Agonist, for the Treatment of Type 2 Diabetes (Poster Hall (Halls D-E); Board No. 112) -  May 11, 2022 - Abstract #ADA2022ADA_1885;    
    Fasiglifam induced a significant accumulation of GCA at 4 µM lower than the human Cmax of 10 µM, whereas IDG16177 showed no significant accumulation at 1 µM higher than the predicted human Cmax of 0.3 µM.IDG16177 did not have a significant effect in quantitative evaluation of the activity of various transcription factors, whereas treatment with 10 uM fasiglifam for 24 hours significantly increased the activities of peroxisome proliferator activating receptor (PPAR), activator protein 1 (AP-1) and nuclear respiratory factor 2 (NRF2), which were highly correlated with liver disease pathogenesis/progression. Interestingly, treatment with 10 μM IDG16177 for 48 h increased the activity of FXR, a master regulator of BA metabolism that inhibits BA absorption system and BA synthesis and promotes BA enterohepatic circulation, by 1.58-fold.These results show that IDG16177 has the advantage of having a low DILI potential compared to fasiglifam in addition to its potent efficacy for the treatment of type 2 diabetes.