Nilapani is a highly selective inhibitor of poly (adenosine diphosphate ribose) polymerase (PARP), which interferes with the DNA damage repair mechanism of tumor cells by inhibiting the activity of PARP-1 and PARP-2 enzymes, thereby inducing synthetic lethal effects. It has significant anti-tumor effects, especially on tumor cells with homologous recombination repair defects (HRD).

1、 Drug name

1. Common name: Niraparib

2. Product Name: Zejula

2、 Indications

Used to treat metastatic castration resistant prostate cancer (mCRPC) with adult BRCA mutations (BRCAm), it needs to be used in combination with prednisone. Patient selection should be based on FDA approved companion diagnostic testing.

3、 Specifications and characteristics

1. Tablets: 100mg

2. Main ingredients: Nilapani tosylate hydrate and abiraterone acetate, excipients include colloidal silica, cross-linked polyvinylpyrrolidone, etc. [16].

4、 Usage and dosage

1. Recommended dosage: Take 200mg of nirapani/1000mg of abiraterone acetate orally once daily, in combination with 10mg of prednisone, until disease progression or intolerable toxicity occurs. It should be taken on an empty stomach (2 hours before meals and 1 hour after meals).

2. Missing service handling: If missed on the same day, it can be replenished as soon as possible; The next day, the regular dosage will be restored without the need for double dosage.

3. For those with swallowing difficulties: The pill can be dissolved in non carbonated water and stirred before taking. The residue needs to be rinsed before drinking.

5、 Dose adjustment

1. Hematological toxicity:

Suspend administration when hemoglobin<8g/dL or platelet<100000/mcL, and reduce to 100mg/1000mg once daily after recovery.

Pause when neutrophils are less than 1000/mL, and reduce after recovery.

2. Hepatotoxicity: Permanently discontinue medication when ALT/AST>5 × ULN or bilirubin>3 × ULN.

3. Non hematological toxicity: If the toxicity level is ≥ 3, the medication will be temporarily suspended. If it does not recover within 28 days, the medication will be permanently discontinued.

6、 Medication precautions

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: tested every two weeks for the first three months, and once a month thereafter.

(3) Hypertension and hypokalemia: Monitor blood pressure and potassium levels weekly, especially in the first two months.

7、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation. Male patients need to use contraception for 4 months after discontinuing the medication.

2. Liver injury: Avoid use in patients with moderate to severe (Child Pugh B/C).

3. Renal injury: Severe patients need to be closely monitored for adverse reactions.

8、 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).

9、 Contraindications

There are no clear contraindications.

10、 Drug interactions

1. Avoid using strong CYP3A4 inducers (such as rifampicin) in combination.

2. CYP2D6 substrates (such as desipramine) need to be reduced to avoid toxicity.

11、 Storage method

Store at room temperature of 20-25 ° C and allow short-term exposure to an environment of 15-30 ° C. Pregnant women who come into contact with pills should wear gloves.

Niraparibinformation