IDH1 Targeting as a New Potential Option for Intrahepatic Cholangiocarcinoma Treatment—Current State and Future Perspectives
Abstract
1. Cholangiocarcinoma: From Classification to Treatment Strategies
2. Molecular Profile of iCCA
IDH1 Mutations in Intrahepatic Cholangiocarcinoma
3. Biological Impact of IDH1 Mutation in Cellular Processes and Its Contribution to Carcinogenesis
3.1. The Role of Wild-Type IDH1 in Cellular Processes
3.2. Biological Effects of Neomorphic Activity of Mutated IDH1
3.3. Biological Impact of IDH1 Mutation in Intrahepatic Cholangiocarcinoma
4. IDH1 Inhibitors for Intrahepatic Cholangiocarcinoma Treatment
5. Future Perspectives of IDH1 Inhibitors Use in Intrahepatic Cholangiocarcinoma
Author Contributions
Funding
Conflicts of Interest
References
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IC50 (µM) | ||||||
---|---|---|---|---|---|---|
Drug | IDH1 Mutation | Mutant | Wild-Type | Ref | Clinical Trial Number | Phase |
AG-120 | R132H R132C R132G R132L R132S | 0.012 0.013 0.008 0.013 0.012 | 0.072 | [124] | NCT02073994 NCT02989857 NCT04088188 2015-005117-72 | I III I III |
IDH305 | R132H R132C | 0.027 0.028 | 6.14 | [125] | NCT02381886 | I |
FT-2102 | R132H R132C | 0.0212 0.0094 | >20.0 | [126] | NCT03684811 2018-001796-21 | I/II Ib/II |
BAY1436032 | R132H R132C R132G R132L R132S | 0.015 0.015 0.004 * 0.003 * 0.016 * | 20.0 | [127,128] | NCT02746081 |
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Crispo, F.; Pietrafesa, M.; Condelli, V.; Maddalena, F.; Bruno, G.; Piscazzi, A.; Sgambato, A.; Esposito, F.; Landriscina, M. IDH1 Targeting as a New Potential Option for Intrahepatic Cholangiocarcinoma Treatment—Current State and Future Perspectives. Molecules 2020, 25, 3754. https://doi.org/10.3390/molecules25163754
Crispo F, Pietrafesa M, Condelli V, Maddalena F, Bruno G, Piscazzi A, Sgambato A, Esposito F, Landriscina M. IDH1 Targeting as a New Potential Option for Intrahepatic Cholangiocarcinoma Treatment—Current State and Future Perspectives. Molecules. 2020; 25(16):3754. https://doi.org/10.3390/molecules25163754
Chicago/Turabian StyleCrispo, Fabiana, Michele Pietrafesa, Valentina Condelli, Francesca Maddalena, Giuseppina Bruno, Annamaria Piscazzi, Alessandro Sgambato, Franca Esposito, and Matteo Landriscina. 2020. "IDH1 Targeting as a New Potential Option for Intrahepatic Cholangiocarcinoma Treatment—Current State and Future Perspectives" Molecules 25, no. 16: 3754. https://doi.org/10.3390/molecules25163754
APA StyleCrispo, F., Pietrafesa, M., Condelli, V., Maddalena, F., Bruno, G., Piscazzi, A., Sgambato, A., Esposito, F., & Landriscina, M. (2020). IDH1 Targeting as a New Potential Option for Intrahepatic Cholangiocarcinoma Treatment—Current State and Future Perspectives. Molecules, 25(16), 3754. https://doi.org/10.3390/molecules25163754