NIRANIB Niraparib capsules 100mg

English Name: Niraparib

Chinese Name: Niraparib

Brand Name: Niranib

Dosage/Specification: 100 mg/capsule, 30 capsules/bottle

Manufacturer: Everest Pharmaceuticals (Bangladesh)

Indications:

This product is indicated for the treatment of recurrent epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer in patients who have responded to platinum-based chemotherapy.

Dosage and Administration:

Dosage and administration may vary depending on the dosage form and specification; please refer to the specific drug package insert or follow a physician's instructions.

1. The recommended dose is 300 mg, taken once daily, either with or without food. Capsules should be swallowed whole at the same time each day. Taking the medication at bedtime may reduce the incidence of nausea. Treatment should begin within 8 weeks of completing a platinum-based chemotherapy regimen. If a dose is missed or vomiting occurs after administration, do not take a replacement dose; simply take the next dose at the scheduled time.

2. If Grade ≥3 non-hematologic adverse reactions occur, suspend treatment. If the adverse reaction resolves within 28 days, resume treatment at a dose of 200 mg. If Grade ≥3 non-hematologic adverse reactions recur at this dose, suspend treatment again; if the reaction resolves within 28 days, resume treatment at 100 mg. If Grade ≥3 non-hematologic adverse reactions recur at this dose and do not resolve within 28 days, discontinue treatment permanently.

3. Upon the first occurrence of a platelet count <100,000/μL or hemoglobin <9 g/dL, reduce the dose to 200 mg and resume treatment. If the condition recurs, suspend treatment; if the neutrophil count recovers to >1,000/μL or hemoglobin recovers to >9 g/dL within 28 days, reduce the dose to 100 mg and resume treatment. If the neutrophil count fails to recover to >1000/μl or hemoglobin to >9 g/dl within 28 days, or if the neutrophil count remains <1000/μl or hemoglobin <8 g/dl at the 100 mg dose level, the drug should be permanently discontinued.

5. If the platelet count drops to ≤10,000/μl, platelet transfusion should be considered; if the patient is concurrently taking antiplatelet or anticoagulant drugs, discontinuation of these concomitant medications or transfusion of a higher dose of platelets should be considered.

Adverse Reactions:

1. Serious adverse reactions include myelodysplastic syndrome and/or acute lymphoblastic leukemia, bone marrow suppression, and cardiotoxicity.

2. Common adverse reactions include thrombocytopenia, anemia, neutropenia, leukopenia, palpitations, nausea, constipation, vomiting, abdominal pain, stomatitis, diarrhea, dyspepsia, dry mouth, fatigue, decreased appetite, urinary tract infection, elevated ALT and/or AST, myalgia, back pain, arthralgia, headache, dizziness, sensory disturbances, insomnia, anxiety, nasopharyngitis, dyspnea, cough, rash, hypertension, and decreased hemoglobin.

3. Uncommon adverse reactions include tachycardia, peripheral edema, hypokalemia, bronchitis, conjunctivitis, elevated GGT, elevated serum creatinine, elevated alkaline phosphatase, weight loss, depression, and epistaxis.

Contraindications:

1. Contraindicated in pregnant women.

2. It is unknown whether the drug is excreted in breast milk; given its serious adverse reactions, breastfeeding women should discontinue breastfeeding during treatment and for at least one month after treatment ends.

3. Safety and efficacy in children have not been established.

4. No dose adjustment is required for patients with mild to moderate renal impairment; safety and efficacy in patients with severe renal impairment or end-stage renal disease have not been established.

5. No dose adjustment is required for patients with mild hepatic impairment; safety in patients with moderate to severe hepatic impairment has not been established. Precautions:

1. This product may cause myelodysplastic syndrome and/or acute lymphoblastic leukemia; severe cases can be fatal. If these conditions are diagnosed, the drug must be discontinued immediately.

2. This product may cause myelosuppression. Complete blood counts should be monitored weekly during the first month of treatment and monthly thereafter; additional testing should be performed as clinically indicated.

3. This product may cause hypertension or even hypertensive crisis. Blood pressure and heart rate should be monitored monthly during the first year of treatment and periodically thereafter. Patients with coronary insufficiency, cardiac arrhythmia, or hypertension require closer monitoring; dosage adjustments of antihypertensive medications may be necessary for patients with hypertension.

4. This product is embryotoxic. Women of childbearing potential must use effective contraceptive measures during treatment and for at least 6 months after treatment ends.

Drug Interactions:

No drug interaction studies have been conducted. Following the recommended oral dose, neither the drug nor its metabolites affect the CYP system, nor are they substrates for P-glycoprotein.

Pharmacology:

This product is an inhibitor of PARP enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, including DNA transcription, cell cycle regulation, and DNA repair. By inhibiting PARP activity and promoting the formation of PARP-DNA complexes, this product disrupts cellular homeostasis, ultimately leading to cell death.

Pharmacokinetics:

1. Absorption: Following a single oral dose of 300 mg, the Cmax is 804 (±403) ng/mL. Within the 30–400 mg dose range, AUC and Cmax are proportional to the dose. The accumulation ratio after 21 days of oral administration is approximately 2-fold. Oral bioavailability is approximately 73%, with peak plasma concentrations reached in about 3 hours; high-fat meals do not affect absorption.

2. Distribution: The apparent volume of distribution is 1220 (±1114) L; studies in cancer patients showed an apparent volume of distribution of approximately 1074 L, and the plasma protein binding rate is 83%. 3. Metabolism: This product is primarily metabolized by carboxylesterases into inactive metabolites; these metabolites undergo further metabolism via glucuronidation.

4. Elimination: Following multiple 300 mg doses, the mean half-life (t½) is 36 hours, and the mean clearance rate in patients with tumors is 16.2 L/h. After administration of radiolabeled drug, 47.5% (range: 33.4%–60.2%) of the radioactivity was recovered in urine and 38.8% (range: 28.3%–47.0%) in feces over a 21-day period. Unchanged drug recovered in urine and feces accounted for 11% and 19% of the administered dose, respectively.

Storage:

Store at 20–25°C; short-term transport at 15–30°C is permitted.

Specifications:

Product Name: Niraparib Capsules (NIRANIB) 100 mg × 30 capsules

Common Name: Niraparib Capsules

Active Ingredient: Niraparib

Dosage Form: Capsule

Specification: 100 mg/capsule, 30 capsules/bottle

Manufacturer: Everest Pharmaceuticals (Bangladesh)

Indications: This product is indicated for the treatment of recurrent epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer in patients who have responded to platinum-based chemotherapy.

Dosage and Administration: Dosage and administration may vary depending on the specific dosage form and strength; please refer to the specific drug package insert or follow medical advice.

1. The recommended dose is 300 mg taken once daily, either with or without food. Capsules should be swallowed whole at the same time each day. Taking the medication at bedtime may reduce the incidence of nausea. Treatment with this product should be initiated within 8 weeks of completing a platinum-based chemotherapy regimen. If a dose is missed or vomiting occurs after administration, do not take a replacement dose; simply take the next dose at the scheduled time. 2. If a non-hematologic adverse reaction of Grade ≥3 occurs, suspend treatment. If the adverse reaction resolves within 28 days, resume treatment at a dose of 200 mg. If a non-hematologic adverse reaction of Grade ≥3 recurs at this dose, suspend treatment; if it resolves within 28 days, resume treatment at 100 mg. If a non-hematologic adverse reaction of Grade ≥3 recurs at this dose and does not resolve within 28 days, permanently discontinue the drug.

3. Upon the first occurrence of a neutrophil count ≤1,000/μL or hemoglobin ≤9 g/dL, reduce the dose to 200 mg and resume treatment. If the condition recurs, suspend treatment; if the neutrophil count recovers to >1,000/μL or hemoglobin recovers to >9 g/dL within 28 days, reduce the dose to 100 mg and resume treatment. If the neutrophil count fails to recover to >1,000/μL or hemoglobin to >9 g/dL within 28 days, or if the neutrophil count remains <1,000/μL or hemoglobin <8 g/dL at the 100 mg dose, permanently discontinue the drug.

5. If the platelet count drops to ≤10,000/μL, consider platelet transfusion. If the patient is concurrently taking antiplatelet or anticoagulant drugs, consider discontinuing these concomitant medications or administering a higher dose of platelets.