Niraparib
Generic Name: niraparib
Brand Names:
Zejula
11 DESCRIPTION Niraparib is an orally available poly (ADP-ribose) polymerase (PARP) inhibitor. The chemical name for niraparib tosylate monohydrate is 2-{4-[(3S)-piperidin-3-yl]phenyl}- 2H -indazole 7-carboxamide 4-methylbenzenesulfonate hydrate (1:1:1). The molecular formula is C 26 H 30 N 4 O 5 S and it has a molecular weight of 510.61 amu. The molecular structure is shown below: Niraparib tosylate monohydrate is a white to off-white, non-hygroscopic crystalline solid.
Overview
11 DESCRIPTION Niraparib is an orally available poly (ADP-ribose) polymerase (PARP) inhibitor. The chemical name for niraparib tosylate monohydrate is 2-{4-[(3S)-piperidin-3-yl]phenyl}- 2H -indazole 7-carboxamide 4-methylbenzenesulfonate hydrate (1:1:1). The molecular formula is C 26 H 30 N 4 O 5 S and it has a molecular weight of 510.61 amu. The molecular structure is shown below: Niraparib tosylate monohydrate is a white to off-white, non-hygroscopic crystalline solid.
Uses
1 INDICATIONS AND USAGE 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. ( 1.1 , 2.1 ) • for the maintenance treatment of adult patients with deleterious or suspected deleterious germline BRCA -mutated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy.
Dosage
2 DOSAGE AND ADMINISTRATION • 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.
Side Effects
6 ADVERSE REACTIONS 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.
Warnings
5 WARNINGS AND PRECAUTIONS • 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. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
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 )] .
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING ZEJULA is available as oval-shaped, film-coated tablets containing 100 mg, 200 mg, or 300 mg of niraparib free base. ZEJULA 100-mg tablets are gray, debossed with “100” on one side and “Zejula” on the other side. Bottle of 30 tablets (NDC 0173-0909-13). ZEJULA 200-mg tablets are blue, debossed with “200” on one side and “Zejula” on the other side.
Frequently Asked Questions
What is Niraparib used for?▼
1 INDICATIONS AND USAGE 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. ( 1.1 , 2.1 ) • for the maintenance treatment of adult patients with deleterious or suspected deleterious germline BRCA -mutated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy.
What are the side effects of Niraparib?▼
6 ADVERSE REACTIONS 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.
Can I take Niraparib during pregnancy?▼
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 )] .
What are the important warnings for Niraparib?▼
5 WARNINGS AND PRECAUTIONS • 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. 4 CONTRAINDICATIONS None. None. ( 4 )
Related Medications
Lidocaine - 3.9%
lidocaine - 3.9%
Amide Local Anesthetic [EPC]
Purpose Topical Pain Reliever
Celtis Occidentalis
celtis occidentalis
Dosage form: SOLUTION. Route: INTRADERMAL, PERCUTANEOUS, SUBCUTANEOUS. Active ingredients: CELTIS OCCIDENTALIS POLLEN (20000 [PNU]/mL). Category: BLA.
.alpha.-tocopherol Acetate, Dl-
.alpha.-tocopherol acetate, dl-
Dosage form: OIL. Active ingredients: .ALPHA.-TOCOPHEROL ACETATE, DL- (1 kg/kg). Category: BULK INGREDIENT.
Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.