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Niraparib

An oral PARP inhibitor (poly(ADP-ribose) polymerase.

PARP enzymes work to repair DNA.

Works to inhibit PARP-1 and PARP-2 enzymes causing increased formation of PARP-DNA complexes that ultimately lead to DNA damage, apoptosis, and cellular death.

Significantly prolong progression free survival in patients with recurrent platinum sensitive ovarian cancer regardless of BRCA status and homologous recombination deficiency status.(PRIMA trial).

Trade name Zejula.

Indicated for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial remission or partial response to platinum-based chemotherapy.

Approval based on the NOVA trial.

Patients with BRCA mutation with recurrent epithelial ovarian, fallopian tube, primary peritoneal disease and estimated median progression free survival of 21 months versus 5.5 months for those who receive placebo.

BRAC Analysis CDx approved identifies patients with a germ line BRCA mutation who are most likely to benefit from niraparib maintenance therapy.

In patients with out this mutation who received this drug had a progression free survival of 9.3 months versus 3.9 months for those who receive placebo.

The combination of bevacizumab plus nirapib in women with relapsed platinum sensitive epithelial ovarian cancer had an objective response rate of 45%.

Nniraparib is a poly (ADP-ribose) polymerase inhibitor, for the treatment of adult patients with advanced homologous recombination deficiency?positive ovarian, fallopian tube, or primary peritoneal cancer who have received ?3 previous lines of chemotherapy.

Homologous recombination deficiency?positive status is defined by a BRCA mutation, or genomic instability and disease progression >6 months after response to the last platinum-based chemotherapy.

Phase 2 multicenter, open-label, single-arm QUADRA clinical trial of 98 patients with advanced ovarian cancer with homologous recombination deficiency?positive tumors as determined by a companion diagnostic, Myriad Genetics� myChoice CDx.

Treatment with niraparib elicited an overall response rate of 24% and an estimated median duration of response of 8.3 months.

Adverse reactions in the QUADRA trial led to dose reduction or int2242uption in 73% of patients receiving niraparib.

The most common adverse reactions (>5%) resulting in dose reduction or int2242uption were: thrombocytopenia (40%), anemia (21%), neutropenia (11%), nausea (13%), vomiting (11%), fatigue (9%), and abdominal pain (5%).

Associated with myelodysplastic syndrome, pancytopenias.

Monitoring of CBCs weekly for the first month, monthly for the next 11 months of treatment and periodically thereafter.

May cause hypertension.

Three 100 mg tablets taken once daily.

Treatment should be started no later than 8 weeks after their most recent platinum containing regimen.

Side effects include: pancytopenia, palpitations, hypertension, nausea, vomiting, constipation, abdominal pain, mucositis, diarrhea, dry mouth, decreased appetite, fatigue, cough, dyspnea, rash, UTIs, elevated liver and resigns, headaches, dizziness, insomnia, and anxiety.

About 1% of patients subsequently developed either myelodysplastic syndrome or acute myelogenous leukemia.

Now approved for treatment of patients with BRCA 1/2-mutant metastatic castration resistant prostate cancer who have previously received taxane based therapy and androgen receptor inhibitor.

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