Generic
Niraparib
1 brands available in the market
At a glance
Niraparib is a PARP inhibitor used for maintenance treatment of recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer. It inhibits PARP enzymes to cause DNA damage and cell death.
Description
Niraparib is an inhibitor of PARP-1 and PARP-2 enzymes which play a role in DNA repair. In vitro studies show 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.
Indications
- Maintenance treatment of recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer (in complete or partial response to platinum-based chemotherapy)
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
PARP Inhibitor
Pharmacology
Niraparib inhibits PARP-1 and PARP-2 enzymes to prevent DNA repair, resulting in DNA damage and apoptosis. It increases cytotoxicity in tumor cell lines with or without BRCA1/2 deficiencies.
Mechanism of action
Causes cancer cell death by inhibiting DNA repair.
Dosage
Adult Dose (Oral):
- 300 mg (three 100 mg capsules) once daily
- Continue until disease progression or unacceptable toxicity
- Start within 8 weeks of platinum-based chemotherapy
Administration
- Swallow capsules whole
- Take at approximately the same time each day
- May take with or without food
- Bedtime administration may help manage nausea
Missed dose
If you miss a dose, take at next scheduled time; do not take additional dose.
Side effects
Common Side Effects (>10%):
- Nausea (74%)
- Thrombocytopenia (61%)
- Fatigue/asthenia (57%)
- Anemia (50%)
- Constipation (40%)
- Vomiting (34%)
- Abdominal pain/distention (33%)
- Neutropenia (30%)
- Insomnia (27%)
- Headache (26%)
- Hypertension (20%)
- Diarrhea (20%)
Serious: MDS/AML, bone marrow suppression, hypertensive crisis
Precautions & warnings
- Discontinue if MDS/AML is confirmed
- May cause bone marrow suppression; monitor CBC regularly (weekly first month, monthly next 11 months)
- Hypertension and hypertensive crisis may occur; monitor BP monthly for first year
- Can cause fetal harm; use effective contraception
Contraindications
- Hypersensitivity
- Breastfeeding
Drug interactions
- CYP3A4 inhibition: caution needed (ciclosporin, tacrolimus, alfentanil, ergotamine, pimozide, quetiapine, halofantrine)
- CYP1A2 induction: caution needed (clozapine, theophylline, ropinirole)
Food interactions
Food does not affect absorption.
Use in pregnancy
Use in Pregnancy: Niraparib is highly unsafe during pregnancy; definite evidence of severe fetal harm. Do not use.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Niraparib is contraindicated during breastfeeding; do not breastfeed for 1 month after final dose.
Pediatric use
Safety and efficacy not established in children under 18 years.
Geriatric use
No dose adjustment needed in patients ≥65 years; limited data in patients ≥75 years.
Renal / hepatic impairment
Renal Impairment: Mild-moderate (CrCl ≥30 mL/min): No dose adjustment needed; Severe or ESRD: Not studied.
Hepatic Impairment: Mild-moderate: No dose adjustment needed; Severe: Caution.
Overdose effects
No specific treatment for overdose; symptomatic supportive measures.
Storage conditions
Store in a cool and dry place; do not store above 30°C; do not use if exposed to temperatures >40°C.
Chemical structure
Niraparib