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About ZEJULA (niraparib)

ZEJULA Inhibits PARP1 and PARP2, Leading to Cancer Cell Death in Pre-Clinical Studies1

ZEJULA is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, PARP1 and PARP2, which play a role in DNA repair.1 In vitro studies suggest that the cytotoxic effects of ZEJULA may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.1

BRCA1/2, breast cancer susceptibility genes 1 and 2.

Preclinical studies suggest the activity of PARP inhibitors depends on tumor exposure and subsequent PARP1/2 inhibition.5

  • Tumor cells carrying a BRCA mutation have been shown to be significantly more sensitive to PARP inhibition than tumors that do not carry a BRCA mutation6
  • It is hypothesized that in tumors without a BRCA mutation, PARP inhibitors may need to achieve higher tumor concentrations for effect6

References: 1. ZEJULA (niraparib). Prescribing Information. GlaxoSmithKline; 2020. 2. Satoh MS, Lindahl T. Role of poly(ADP-ribose) formation in DNA repair. Nature. 1992;356(6367):356-358. 3. Rein ID, Landsverk KS, Micci F, Patzke S, Stokke T. Replication-induced DNA damage after PARP inhibition causes G2 delay, and cell line-dependent apoptosis, necrosis and multinucleation. Cell Cycle. 2015;14(20):3248-3260. 4. Data on file, GlaxoSmithKline. 5. Ricks TK, Chiu HJ, Ison G, et al. Successes and challenges of PARP inhibitors in cancer therapy. Front Oncol. 2015;5:222. doi: 10.3389/fonc.2015.00222. 6. Farmer H, McCabe N, Lord CJ, et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature. 2005;434(7035):917-921.

Efficacy data


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Study design


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