Pamiparib

Pamiparib is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC₅₀s = 1.3 and 0.92 nM, respectively).¹ It is selective for PARP1 and PARP2 over PARP3 (IC₅₀ = 0.068 µM) and other PARP isoforms (IC₅₀s = 2.4->100 µM), as well as over tankyrase 1 (TNKS1) and TNKS2 (IC₅₀s = 0.23 and 0.14 µM, respectively). Pamiparib inhibits PARP activity induced by hydrogen peroxide in HeLa cells with an IC₅₀ value of 0.24 nM. It selectively inhibits proliferation of MDA-MB-436 cells expressing mutant BRCA1 and Capan-1 cells expressing mutant BRCA2 (EC₅₀s = 41 and 960 nM, respectively) over MDA-MB-231 cells expressing wild-type BRCA (EC₅₀ = ~9,000 nM). Pamiparib (1.6-6.3 mg/kg twice per day) induces tumor regression in an MDA-MB-436 mouse xenograft model. It also potentiates increases in survival induced by temozolomide (Item No. 14163) in an H209 mouse xenograft model of small cell lung cancer brain metastasis.

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1. Xiong, Y., Guo, Y., Liu, Y., et al. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor. Neoplasia 22(9), 431-440 (2020).