Niraparix

Niraparib (Niraparib) Introduction

Common name: Niraparib

Commercial name: Niraparib

All names: Niraparib, Niraparib, Zejula, MK-4827

Niraparib Indications

Niraparib is a poly(ADP-ribose) polymerase (PARP) inhibitor indicated for the maintenance treatment of adult patients with recurrent epidermal ovarian cancer, fallopian tube cancer, and primary peritoneal cancer (who need to have a complete or partial response to platinum-based chemotherapy).

Niraparib dosage and administration

1. The recommended dose is 300 mg once a day with or without food.

2. Continue treatment until disease progression or unacceptable adverse reactions.

3. For adverse reactions, consider interrupting treatment, reducing the dose or discontinuing administration.

Niraparib drug introduction

September 18, 2017, niraparib: Developed by Tesaro, this drug is an oral poly ADP ribose polymerase (PARP) inhibitor that exploits defects in the DNA repair pathway to preferentially kill cancer cells. This mode of action gives niraparib the potential to treat a broad range of tumor types with DNA repair defects. PARP is associated with a wide range of tumor types, particularly breast and ovarian cancer.

Specifically, the CHMP recommends approval of Zejula as monotherapy for the treatment of adult patients with platinum-sensitive recurrent high-grade serous epithelial ovarian, fallopian tube, or primary peritoneal cancer who have achieved a complete or partial response to platinum-containing chemotherapy.

Niraparib is the first and only PARP inhibitor that does not differentiate between BRCA gene mutations or biomarkers.

Niraparib mechanism of action

Niraparib is a poly(ADP-ribose) polymerase (PARP) enzyme, an inhibitor of PARP-1 and PARP-2, which play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzyme activity and increased formation of PARP-DNA complexes leading to DNA damage, apoptosis, and cell death. Increased niraparib-induced cytotoxicity was observed in tumor cell lines with or without defects in BRCA1/2. Niraparib reduced tumor growth in a xenograft model of BRCA1/2-deficient mouse tumor cells and in a human patient-derived xenograft tumor model with homologous recombination with either mutant or wild-type BRCA1/2 deficiency.

Niraparib dosage forms and specifications

Capsules: 100mg

Niraparib contraindications

None.

Niraparib Warnings and Precautions

Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): MDS/AML has occurred in patients exposed to ZEJULA, and in some cases sensitization has occurred. Monitor patients for hematologic toxicities and discontinuation if MDS/AML is confirmed.

Adverse reactions of niraparib

The most common adverse reactions (incidence ≥10%) are thrombocytopenia, anemia, neutropenia, leukopenia, palpitations, nausea, constipation, vomiting, abdominal pain/bloating , mucositis/gastritis, diarrhea, indigestion, dry mouth, fatigue/asthenia, decreased appetite, urinary tract infection, elevated AST/ALT, myalgia, back pain, arthralgia, headache, dizziness, dysgeusia, insomnia, anxiety, nasopharyngitis, dyspnea, cough, rash and hypotension.

Niraparib use in special populations

Breastfeeding: Women are advised not to breastfeed during treatment and for 1 month after the last dose.