bioRxiv· Tan, P. W., Hernandez Martin, N., Esposito-Zapero, C., Sun, C., Toyonaga, T., Zheng, M.-Q., Kapinos, M., Thomas, M. A., Nejati, S. F., Korsah, C., Holden, D., Chen, B., Sepulcre, J., Carson, R. E., Huang, Y., De Feyter, H. M., Cai, Z. ·· 19 hours agoScore47
Preclinical Evaluation of Itareparib, a brain penetrant PARP1-selective radioligand, in Glioma Rat Model and Nonhuman Primate
In brief
Preclinical evaluation of [18F]Itareparib showed tumor uptake 4-fold higher than contralateral brain tissue in an orthotopic BT142 IDH1-mutant glioma rat model; uptake fell 77% after blocking with the PARP1-selective inhibitor AZD9574. In nonhuman primates, blocking reduced VT by 21%±6%, and the parent tracer fraction in rat brain exceeded 99% at 60 minutes. The results support further development of [18F]Itareparib for quantitative PET imaging of PARP1 in brain tumors.
Source: bioRxiv