Preclinical Evaluation of Itareparib, a brain penetrant PARP1-selective radioligand, in Glioma Rat Model and Nonhuman Primate
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Preclinical evaluation of [18F]Itareparib showed tumor uptake 4-fold higher than contralateral brain tissue in an orthotopic BT142 IDH1-mutant glioma rat model, with uptake reduced 77% by blocking with the PARP1-selective inhibitor AZD9574. In nonhuman primates, blocking reduced VT by 21%±6%, and in rats the parent tracer fraction in brain exceeded 99% at 60 minutes. The results support further development of [18F]Itareparib for quantitative PET imaging of PARP1 in brain tumors.
Excerpted from bioRxiv
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- bioRxivPickPreclinical Evaluation of Itareparib, a brain penetrant PARP1-selective radioligand, in Glioma Rat Model and Nonhuman Primate
Preclinical evaluation of [18F]Itareparib showed tumor uptake 4-fold higher than contralateral brain tissue in an orthotopic BT142 IDH1-mutant glioma rat model, with uptake reduced 77% by blocking with the PARP1-selective inhibitor AZD9574. In nonhuman primates, blocking reduced VT by 21%±6%, and in rats the parent tracer fraction in brain exceeded 99% at 60 minutes. The results support further development of [18F]Itareparib for quantitative PET imaging of PARP1 in brain tumors.
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