pharmacopeia
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/api/v1/drug/niraparib

Mechanism of action

Sourced from openFDA

Niraparib is an inhibitor of PARP enzymes, including PARP-1 and PARP-2, that play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.

Poly(ADP-Ribose) Polymerase

Indications

Sourced from openFDA
  • ZEJULA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: • for the maintenance treatment of adult patients with advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to first-line platinum-based chemotherapy and whose cancer is associated with homologous recombination deficiency (HRD)-positive status defined by either: o a deleterious or suspected deleterious BRCA mutation, and/or o genomic instability. Select patients for therapy based on an FDA‑authorized companion diagnostic for ZEJULA.

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

• First‑Line Maintenance Treatment of HRD‑Positive Advanced Ovarian Cancer: o For patients weighing <77 kg (<170 lbs) OR with a platelet count <150,000/mcL, the recommended dosage is 200 mg taken orally once daily. ( 2.2 ) o For patients weighing ≥77 kg (≥170 lbs) AND a platelet count ≥150,000/mcL, the recommended dosage is 300 mg taken orally once daily. ( 2.2 ) • Maintenance Treatment of Recurrent Germline BRCA‑Mutated Ovarian Cancer: The recommended dosage is 300 mg taken orally once daily. ( 2.2 ) • Continue treatment until disease progression or unacceptable toxicity. ( 2.2 ) • ZEJULA may be taken with or without food. ( 2.2 ) • For adverse reactions, consider interruption of treatment, dose reduction, or dose discontinuation. ( 2.3 ) • For patients with moderate hepatic impairment, recommended dosage is 200 mg taken orally once daily. ( 2.4 ) 2.1 Patient Selection First-Line Maintenance Treatment of HRD-Positive Advanced Ovarian Cancer Select patients for first-line maintenance treatment of advanced ovarian cancer with ZEJULA based on the presence of HRD defined by either a deleterious or suspected deleterious BRCA mutation, and/or genomic instability [see Clinical Studies ( 14.1 )] . Information on FDA‑authorized tests for the detection of HRD‑positive status for this indication is available at https://www.fda.gov/companiondiagnostics.

Warnings & precautions

Sourced from openFDA

• Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): MDS/AML occurred in patients exposed to ZEJULA, and some cases were fatal. Monitor patients for hematological toxicity and discontinue if MDS/AML is confirmed. ( 5.1 ) • Bone Marrow Suppression: Test complete blood counts weekly for the first month, monthly for the next 11 months, and periodically thereafter for clinically significant changes. ( 5.2 ) • Hypertension and Cardiovascular Effects: Monitor blood pressure and heart rate at least weekly for the first 2 months, then monthly for the first year and periodically thereafter during treatment with ZEJULA. Manage with antihypertensive medications and adjustment of the dose of ZEJULA, if necessary. ( 5.3 ) • Posterior Reversible Encephalopathy Syndrome (PRES): PRES has occurred in patients treated with ZEJULA. Discontinue ZEJULA if PRES is confirmed. ( 5.4 ) • Embryo-Fetal Toxicity: ZEJULA can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.5 , 8.1 , 8.3 ) 5.1 Myelodysplastic Syndrome/Acute Myeloid Leukemia Myelodysplastic syndrome/acute myeloid leukemia (MDS/AML), including cases with a fatal outcome, have been reported in patients who received ZEJULA. In PRIMA, of patients within the HRD-positive population, MDS/AML occurred in 8 out of 245 (3.3%) patients treated with ZEJULA and in 3 out of 125 (2.4%) patients treated with placebo with a follow-up of 6.1 years [see Adverse Reactions ( 6.1 )] .

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: • MDS/AML [see Warnings and Precautions ( 5.1 )] • Bone marrow suppression [see Warnings and Precautions ( 5.2 )] • Hypertension and cardiovascular effects [see Warnings and Precautions ( 5.3 )] • Posterior reversible encephalopathy syndrome [see Warnings and Precautions ( 5.4 )] Most common adverse reactions (incidence ≥10%) in patients who received ZEJULA were nausea, thrombocytopenia, anemia, fatigue, constipation, musculoskeletal pain, abdominal pain, vomiting, neutropenia, decreased appetite, leukopenia, insomnia, headache, dyspnea, rash, diarrhea, hypertension, cough, dizziness, acute kidney injury, urinary tract infection, and hypomagnesemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact GlaxoSmithKline at 1-888-825-5249 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action, ZEJULA can cause fetal harm when administered to pregnant women [see Clinical Pharmacology ( 12.1 )] . There are no data regarding the use of ZEJULA in pregnant women to inform the drug-associated risk. ZEJULA has the potential to cause teratogenicity and/or embryo-fetal death since niraparib is genotoxic and targets actively dividing cells in animals and patients (e.g., bone marrow) [see Warnings and Precautions ( 5.2 ), Nonclinical Toxicology ( 13.1 )] . Due to the potential risk to a fetus based on its mechanism of action, animal developmental and reproductive toxicology studies were not conducted with niraparib. Apprise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. 8.2 Lactation Risk Summary No data are available regarding the presence of niraparib or its metabolites in human milk, or on its effects on the breastfed child or milk production.

Pharmacokinetics

Sourced from openFDA
Metabolism
Niraparib mean (±SD) maximum plasma concentration (C max ) is 603 (±343) ng/mL at the approved maximum recommended dose of 300 mg. Niraparib steady-state C max and AUC increased in a dose-proportional manner with daily doses ranging from 30 mg (0.15 times the approved minimum recommended dose) to 400 mg (1.3 times the approved maximum recommended dose).

Approval history

Sourced from openFDA
  • Apr 26, 2023NDANDA214876Glaxosmithkline
  • Aug 11, 2023NDANDA216793Janssen Biotech

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
21,973 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea5,77426%
  2. 2Fatigue5,23024%
  3. 3Platelet Count Decreased4,11319%
  4. 4Constipation4,10719%
  5. 5Insomnia2,83913%
  6. 6Blood Pressure Increased2,45811%
  7. 7Headache2,36911%
  8. 8Off Label Use2,24310%
  9. 9Vomiting2,0329.2%
  10. 10Decreased Appetite1,8808.6%
  11. 11Asthenia1,8568.4%
  12. 12Product Dose Omission Issue1,8558.4%
  13. 13Carbohydrate Antigen 125 Increased1,8488.4%
  14. 14Haemoglobin Decreased1,7437.9%
  15. 15Dizziness1,6027.3%

Clinical trials

View JSON

The 10 most recently updated of 236 ClinicalTrials.gov registrations naming Niraparib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Niraparib work?
Niraparib is an inhibitor of PARP enzymes, including PARP-1 and PARP-2, that play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
What is Niraparib used for?
According to FDA labeling, Niraparib carries indications including: ZEJULA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: • for the maintenance treatment of adult patients with advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to first-line platinum-based chemotherapy and whose cancer is associated with homologous recombination deficiency (HRD)-positive status defined by either: o a deleterious or suspected deleterious BRCA mutation, and/or o genomic instability. Select patients for therapy based on an FDA‑authorized companion diagnostic for ZEJULA.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Niraparib?
Niraparib is classified as Poly (ADP-ribose) polymerase (PARP) inhibitors, Poly(ADP-Ribose) Polymerase Inhibitor, Poly(ADP-Ribose) Polymerase Inhibitors, DNA Alteration, Increased Cellular Death.
What are the brand names for Niraparib?
Niraparib is marketed under brand names including Akeega, Zejula.
What are the contraindications for Niraparib?
Niraparib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for niraparib is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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