Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synt
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.
IDX-1197 potently, selectively inhibits PARP1 and PARP2 activities with no sensitivity to PARP5A (Tankyrase-1), and significantly inhibits PARP1-mediated PAR expression in DNA damage-induced Hela cells.[1]
In the germline BRCA1-mutated ovarian cancer PDX model, oral administration of IDX-1197 exhibits significant PAR inhibition in tumor tissues, and dose-dependently lead to potent tumor growth inhibition compared to Olaparib treatment group.[1]
[1] Myongjae Lee, et al. American Association for Cancer Research, 2018.
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