Niraparib
Niraparib Uses, Dosage, Side Effects, Food Interaction and all others data.
Niraparib is an orally active PARP inhibitor developed by Tesaro to treat ovarian cancer. FDA approval on March 2017.
Cardiovascular Effects:Niraparib has the potential to cause effects on pulse rate and blood pressure in patients receiving the recommended dose, which may be related to pharmacological inhibition of the dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter (SERT).In the NOVA study, mean pulse rate and blood pressure increased over baseline in the niraparib arm relative to the placebo arm at all on-study assessments. Mean greatest increases from baseline in pulse rate on treatment were 24.1 and 15.8 beats/min in the niraparib and placebo arms, respectively. Mean greatest increases from baseline in systolic blood pressure on treatment were 24.5 and 18.3 mmHg in the niraparib and placebo arms, respectively. Mean greatest increases from baseline in diastolic blood pressure on treatment were 16.5 and 11.6 mmHg in the niraparib and placebo arms, respectively.Cardiac ElectrophysiologyThe potential for QTc prolongation with niraparib was evaluated in a randomized, placebo-controlled trial in cancer patients (367 patients on niraparib and 179 patients on placebo). No large changes in the mean QTc interval (>20 ms) were detected in the trial following the treatment of niraparib 300 mg once daily.
| Trade Name | Niraparib |
| Availability | Prescription only |
| Generic | Niraparib |
| Niraparib Other Names | Niraparib |
| Related Drugs | carboplatin, doxorubicin, cisplatin, paclitaxel, Avastin, bevacizumab, Lynparza, Zejula, Alymsys, Zirabev |
| Weight | 100mg |
| Type | Oral capsule |
| Formula | C19H20N4O |
| Weight | Average: 320.396 Monoisotopic: 320.16371128 |
| Protein binding | Niraparib is 83.0% bound to human plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Niraparib is a poly-ADP ribose polymerase inhibitor used to treat recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer responding to platinum based chemotherapy.
Niraparib is indicated for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy
Niraparib is also used to associated treatment for these conditions: Fallopian Tube Cancer, Ovarian Epithelial Cancer, Primary Peritoneal Cancer
How Niraparib works
Niraparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, PARP-1 and PARP-2, which play a role in DNA repair. In vitro studies have shown 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. Increased niraparib-induced cytotoxicity was observed in tumor cell lines with or without deficiencies in BRCA1/2. Niraparib decreased tumor growth in mouse xenograft models of human cancer cell lines with deficiencies in BRCA1/2 and in human patient-derived xenograft tumor models with homologous recombination deficiency that had either mutated or wild type BRCA1/2.
Food Interaction
- Take at the same time every day.
- Take with or without food.
Niraparib Drug Interaction
Moderate: paclitaxel protein-bound, lactobacillus acidophilus, doxorubicin, aspirin, cabozantinib, lactobacillus rhamnosus gg, apixaban, olaparibUnknown: acetaminophen, calcium carbonate, multivitamin with minerals, loratadine, duloxetine, leuprolide, loperamide, loperamide, levothyroxine, dronabinol, ascorbic acid, cholecalciferol
Niraparib Disease Interaction
Moderate: cardiovascular disorders, liver dysfunction, MDS/AML, pancytopenia, renal impairment
Volume of Distribution
The average (±SD) apparent volume of distribution (Vd/F) was 1220 (±1114) L.
Elimination Route
The absolute bioavailability of niraparib is approximately 73%. Following oral administration of niraparib, peak plasma concentration, Cmax, is reached within 3 hours. Concomitant administration of a high fat meal (800-1,000 calories with approximately 50% of total caloric content of the meal from fat) did not significantly affect the pharmacokinetics of niraparib.
Following a single-dose administration of 300 mg niraparib, the mean (±SD) peak plasma concentration (Cmax) was 804 (± 403) ng/mL. The systemic exposures (Cmax and AUC) of niraparib increased in a dose proportional manner with daily doses ranging 30 mg (0.1 times the approved recommended dosage) to 400 mg (1.3 times the approved recommended dosage). The accumulation ratio of niraparib exposure following 21 days of repeated daily doses was approximately 2 fold for doses ranging from 30 mg to 400 mg.
Half Life
Following multiple daily doses of 300 mg niraparib, the mean half-life (t1/2) is 36 hours.
Clearance
the apparent total clearance (CL/F) of niraparib was 16.2 L/h in cancer patients.
Elimination Route
Following administration of a single oral 300 mg dose of radio-labeled niraparib, the average percent recovery of the administered dose over 21 days was 47.5% (range 33.4% to 60.2%) in urine, and 38.8% (range 28.3% to 47.0%) in feces.
Innovators Monograph
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