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Niraparib is a highly selective poly(ADP-ribose) polymerase (PARP) inhibitor that interferes with the DNA damage repair mechanism of tumor cells by inhibiting the activity of PARP-1 and PARP-2 enzymes, thus inducing a synthetic lethal effect. It has a significant anti-tumor effect especially on tumor cells with homologous recombination repair deficiency (HRD).
1. Generic name: Niraparib (Niraparib)
2. Trade name: Zej ula
It is used to treat adult BRCA-mutated (BRCAm) metastatic castration-resistant prostate cancer (mCRPC) and needs to be used in combination with prednisone. Patient selection needs to be based on FDA-approved companion diagnostic tests.
1. Tablet: 100mg
2. Main ingredients: niraparib tosylate-hydrate and abiraterone acetate, excipients include colloidal silica, cross-linked povidone, etc. [16].
1. Recommended dosage: Take 200 mg niraparib/1,000 mg abiraterone acetate orally once a day, combined with 10 mg prednisone, until disease progression or intolerable toxicity. It needs to be taken on an empty stomach (fasting 2 hours before meals and 1 hour after meals).
2. Treatment of missed doses: If you miss a dose on the same day, you can take it as soon as possible; resume the regular dose the next day, no need to double the dose.
3. People with difficulty swallowing: Dissolve the tablets in non-carbonated water and stir before taking. The residue needs to be rinsed before drinking.
1. Hematological toxicity :
Suspend the administration when hemoglobin <8g/dL or platelets <100,000/mcL, and reduce the dose to 100mg/1,000mg once a day after recovery.
Pause when neutrophils <1,000/mcL, and reduce the dose after recovery.
2. Hepatotoxicity : Permanently discontinue the drug when ALT/AST>5×ULN or bilirubin>3×ULN.
3. Non-hematological toxicity : Suspension of administration for grade ≥3 toxicity, and permanent discontinuation if the drug does not recover within 28 days.
1. Medication time : Take strictly on an empty stomach to avoid food affecting absorption.
2. Monitoring requirements :
(1) Hematology: weekly testing in the first month, and once a month thereafter.
(2) Liver function: Test every two weeks in the first 3 months, and once a month thereafter.
(3) Hypertension and hypokalemia : Monitor blood pressure and serum potassium every week, especially in the first 2 months.
1. Pregnant women : Contraindicated as it may cause fetal malformations. Male patients need to use contraception until 4 months after stopping the drug.
2. Patients with liver damage: Avoid use in patients with moderate to severe liver damage (Child-PughB/C).
3. Kidney damage : Severe patients need to be closely monitored for adverse reactions.
1. Common (≥10%): Anemia (28%), thrombocytopenia (8%), fatigue (43%), hypertension (33%), nausea (33%).
2. Serious risks: Myelodysplastic syndrome (MDS/AML), liver failure, posterior reversible encephalopathy syndrome (PRES).
There are no clear contraindications.
1. Avoid combined use of strong CYP3A4 inducers (such as rifampicin).
2. The dosage of CYP2D6 substrates (such as desipramine) needs to be reduced to avoid toxicity.
Stored at room temperature 20-25°C, short-term storage at 15-30°C allowed. Pregnant women should wear gloves when handling tablets.