Pamiparib

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC₅₀ values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor^[1][2]. IC50 & Target:PARP^[1] In Vitro:Pamiparib shows potent DNA-trapping activity with an IC₅₀ of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC₅₀ of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors^[3]. In Vivo:Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models^[4].