pamiparib-maleate

Description: Pamiparib maleate, the maleate salt of pamiparib (also known as BGB-290), is a novel, potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in enzymatic assays. Pamiparib diaplays high selectivity over other PARP enzymes. It has good DMPK (Drug metabolism and pharmacokinetic) profiles. Pamiparib selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway which enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. Pamiparib can potentiate the cytotoxicity of DNA-damaging agents and reverse the chemo- and radioresistance of tumor cells. Pamiparib is currently under clinical investigation and has the potential to be used for the treatment of various cancers including the solid tumor.

References: AACR 106th Annual Meeting 2015; Supplement/1651; AACR 106th Annual Meeting 2015_Supplement/1653; WO 2013097225 A1.