Niraparib, p-Toluenesulfonate Salt

Soluble in DMSO. Niraparib enhanced radiation-induced cytotoxicity in neuroblastoma cells. In vivo treatment with niraparib and radiation prolonged survival of mice in a murine xenograft model of metastatic neuroblastoma when compared to single modalities. Mueller S., et al. 'Poly (ADP-Ribose) polymerase inhibitor MK-4827 together with radiation as a novel therapy for metastatic neuroblastoma.' Anticancer Res. 33: 755-762 (2013). A phase 1 clinical trial demonstrated niraparib inhibited PARP more than 50% at doses greater than 80 mg/day and had antitumour activity at doses beyond 60 mg/day. Antitumour activity of niraparib was reported in BRCA1 or BRCA2 mutation carriers with ovarian cancer, breast cancer, and in patients with sporadic high-grade serous ovarian cancer, non-small-cell lung cancer, and prostate cancer. Sandhu S.K., et al. 'The poly(ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial.' Lancet Oncol. 14: 882-892 (2013).