Zejula(niraparib)
Oncology· 204 cited findings· 2 source documents
Company: GSK plc →
What the regulatory reviews say
Zejula (niraparib) is indicated as monotherapy for the maintenance treatment of adult patients with platinum-sensitive relapsed high-grade serous epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in response (complete or partial) to platinum-based chemotherapy. It received orphan medicinal product designation (EU/3/10/760) and was granted orphan designation in August 2010. The marketing authorisation application was submitted on 4 October 2016, with EMA/CHMP eligibility agreed on 25 June 2015. Regular approval for niraparib was granted on April 29, 2020, with its indication narrowed on December 8, 2022.
Niraparib demonstrates high potency in inhibiting PARP1 (IC50: 1.1 nM) and PARP2 (IC50: 0.4 nM). It also inhibits intracellular PARylation in HeLa cells with an IC50 of 4 nM and in Jurkat cells with an IC50 of 22 nM. In orthotopic high-grade serous ovarian cancer PDX models, the tumour regression rate was 26% across all models and 44% in HRD-positive models. The recommended Phase 2 dose and Maximum Tolerated Dose (MTD) is 300 mg QD.
Safety findings include an incidence of MDS or AML of 3.3% in HRD-positive patients treated with niraparib, compared to 2.4% in the placebo group. More than 70% of patients experienced dose modifications due to adverse events. The IC50 for hERG current inhibition is 10 µM. Oral bioavailability was 27% in rats and 57% in dogs.
Key figures — cited to the source page
| IC50 for PARP1 inhibition | 1.1 nM | GSK plc — Zejula EMA EPAR public assessment report, p.19 |
| IC50 for PARP2 inhibition | 0.4 nM | GSK plc — Zejula EMA EPAR public assessment report, p.19 |
| Tumour regression rate in orthotopic high-grade serous ovarian cancer PDX models (HRD positive models) | 44 % | GSK plc — Zejula EMA EPAR public assessment report, p.22 |
| MDS or AML incidence (Niraparib, HRD-positive) | 3.3 % | GLAXOSMITHKLINE — Zejula FDA Review, p.16 |
| MDS or AML incidence (Placebo, HRD-positive) | 2.4 % | GLAXOSMITHKLINE — Zejula FDA Review, p.16 |
| Dose modifications due to AEs | >70 % | GSK plc — Zejula EMA EPAR public assessment report, p.120 |
| Orphan medicinal product designation | EU/3/10/760 | GSK plc — Zejula EMA EPAR public assessment report, p.7 |
| Regular approval date for niraparib | April 29, 2020 | GLAXOSMITHKLINE — Zejula FDA Review, p.5 |
Source documents
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Figures are as stated in the cited regulatory review documents (different drugs are studied in different trials — values are not head-to-head comparisons). Educational reference only — not medical or investment advice.