MK-4827

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Description

MK-4827 (Niraparib) is an oral potent, selective PARP-1 and PARP-2 inhibitor currently in phase I clinical trials for cancer treatment. MK-4827 shows excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with EC(50) = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range. MK-4827 reduced PAR levels in tumors by 1 h after administration which persisted for up to 24 h. MK-4827 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant.

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