niraparib (Rx)

Brand and Other Names:Zejula
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg

Ovarian Cancer

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

300 mg PO qDay; continue until disease progression or unacceptable toxicity

Also see Administration

Dosage Modifications

Dose reductions

  • First dose reduction: 200 mg/day
  • Second dose reduction: 100 mg/day
  • Discontinue if further dose reduction <100 mg/day is required

Nonhematologic adverse reactions

  • ≥Grade 3 reactions where prophylaxis is not considered feasible or adverse reaction persists despite treatment: Withhold niraparib up to 28 days or until resolution of adverse reactions; resume at a reduced dose (up to 2 dose reductions are permitted)
  • ≥Grade 3 reactions lasting >28 days and taking niraparib 100 mg/day: Discontinue

Hematologic adverse reactions

  • Platelet count <1000,000/mcL
    • First occurrence: Withhold niraparib up to 28 days and monitor blood cell counts weekly until platelets ≥100,000/mcL; resume at same or reduced dose; if platelet count is <75,000/mcL, resume at reduced dose
    • Second occurrence: Withhold niraparib up to 28 days and monitor blood cell counts weekly until platelets ≥100,000/mcL; resume at reduced dose; discontinue if platelet count has not returned to acceptable levels within 28 days or if the patient is already on 100 mg/day
  • Neutrophil count <1000/mcL or hemoglobin <8 g/dL
    • Withhold niraparib up to 28 days and monitor blood cell counts weekly until neutrophils ≥1500/mcL or hemoglobin ≥9 g/dL; resume at reduced dose
    • Discontinue if neutrophils and/or hemoglobin have not returned to acceptable levels within 28 days or if the patient is already on 100 mg/day
  • Hematologic adverse reaction requiring transfusion
    • Platelet count ≤10,000/mcL: Consider platelet transfusion
    • If other risk factors exist (eg anticoagulants, antiplatelets), consider interrupting anticoagulants or antiplatelet drugs and/or transfuse at a higher platelet count
    • Resume niraparib at a reduced dose

Renal impairment

  • Mild-to-moderate (CrCl ≥30 mL/min): No dose adjustment required
  • Severe or ESRD: Not studied

Hepatic impairment

  • Mild: No dose adjustment required
  • Moderate or severe: Not studied

Safety and efficacy not established

Next:

Adverse Effects

Adverse effects include all grades unless otherwise stated

>10%

Nausea (74%)

Thrombocytopenia (61%)

Fatigue/asthenia (57%)

Anemia (50%)

Constipation (40%)

Vomiting (34%)

Abdominal pain/distention (33%)

Neutropenia (30%)

Thrombocytopenia, grades 3 or 4 (29%)

Insomnia (27%)

Headache (26%)

Anemia, grades 3 or 4 (25%)

Nasopharyngitis (23%)

Rash (21%)

Hypertension (20%)

Neutropenia, grades 3 or 4 (20%)

Mucositis/stomatitis (20%)

Diarrhea (20%)

Dyspepsia (20%)

Myalgia (19%)

Back pain (18%)

Dyspepsia (18%)

Dizziness (18%)

Leukopenia (17%)

Cough (16%)

UTI (13%)

Arthralgia (13%)

Anxiety (11%)

1-10%

Palpitations (10%)

Dry mouth (10%)

AST/ALT elevation (10%)

Dysgeusia (10%)

Hypertension, grade 3 or 4 (9%)

Leukopenia, grades 3 or 4 (5%)

Previous
Next:

Warnings

Contraindications

None

Cautions

Myelodysplastic syndrome/acute myeloid leukemia (MDS/AML), including cases with fatal outcome, reported; discontinue drug if MDS/AML is confirmed

May cause bone marrow suppression resulting in hematologic toxicities (eg, thrombocytopenia, anemia, neutropenia); do not initiate until patients have recovered from hematological toxicities caused by previous chemotherapy (grade ≤1); monitor complete blood cell counts weekly for the first month, monthly for the next 11 months of treatment, and periodically after this time (also see Dosage Modifications)

Hypertension and hypertensive crisis reported; monitor BP and HR monthly for the first year and periodically thereafter during treatment; medically manage hypertension with antihypertensive medications and niraparib dose adjustment

Based on its mechanism of action, can cause fetal harm if administered to a pregnant woman (see Pregnancy)

Previous
Next:

Pregnancy

Pregnancy

Niraparib has the potential to cause teratogenicity and/or embryo-fetal death since niraparib is genotoxic and targets actively dividing cells in animals and patients (eg, bone marrow)

A pregnancy test is recommended for females of reproductive potential prior to initiating drug

Based on animal studies, may impair fertility in males of reproductive potential

Contraception

  • Advise females of reproductive potential to use effective contraception during treatment for at least 6 months following the last dose

Lactation

Because of the potential for serious adverse reactions in breastfed infants, advise a lactating woman not to breastfeed during treatment and for 1 month after receiving the final dose

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Previous
Next:

Pharmacology

Mechanism of Action

Poly (ADP-ribose) polymerase (PARP) inhibitor; 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

Absorption

Bioavailability: 73%

Peak plasma time: 3 hr

Peak plasma concentration: 804 ng/mL

Distribution

Protein bound: 83%

Vd: 1200 L

Metabolism

Metabolized primarily by carboxylesterases (CEs) to form a major inactive metabolite, which subsequently undergoes glucuronidation

Elimination

Half-life: 36 hr

Excretion: 47.5% urine; 38.8% feces

Previous
Next:

Administration

Oral Administration

May take with or without food

Initiate niraparib no later than 8 weeks after their most recent platinum-containing regimen

Instruct patient to take dose at about the same time each day

Swallow each capsule whole

Bedtime administration may be a potential method for managing nausea

Missed or vomited dose

  • Take next dose at its regularly scheduled time
  • Do not take an additional dose

Storage

Store at 20-25°C (68-77°F); excursions are permitted between 15-30°C (59-86°F)

Previous
Next:

Images

Previous
Next:

Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
Additional Offers
Email to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Email Forms to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Previous
Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.