Peringatan Keamanan

There is limited information available regarding the acute toxicity profile and overdosage of niraparib.

Niraparib

DB11793

small molecule approved investigational

Deskripsi

Niraparib is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. By blocking the enzymes responsible for DNA repair, niraparib induces cytotoxicity in cancer cells.L43277 Niraparib is selective towards PARP-1 and PARP-2.A253248 First approved by the FDA on March 27, 2017,A253912 niraparib is used to treat epithelial ovarian, fallopian tube, or primary peritoneal cancer.L43277 Niraparib was approved by the European Commission on November 16, 2017 L43742 and by Health Canada on June 27, 2019.L43747

Struktur Molekul 2D

Berat 320.396
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following multiple daily doses of 300 mg of niraparib, the mean half-life (t<sub>1/2</sub>) is 36 hours.[L43277]
Volume Distribusi The average (±SD) apparent volume of distribution (Vd/F) was 1,220 (±1,114) L. In a population pharmacokinetic analysis, the Vd/F of niraparib was 1,074 L in patients with cancer.[L43277]
Klirens (Clearance) In a population pharmacokinetic analysis, the apparent total clearance (CL/F) of niraparib was 16.2 L/h in patients with cancer.[L43277]

Absorpsi

Following a single-dose administration of 300 mg niraparib, the mean (±SD) peak plasma concentration (Cmax) was 804 (±403) ng/mL. The exposure (Cmax and AUC) of niraparib increased in a dose-proportional manner with daily doses ranging from 30 mg (0.1 times the approved recommended dose) to 400 mg (1.3 times the approved recommended dose). The accumulation ratio of niraparib exposure following 21 days of repeated daily doses was approximately 2-fold for doses ranging from 30 to 400 mg. The Tmax is about three hours.L43277 The absolute bioavailability of niraparib is approximately 73%. Food does not appear to affect drug exposure.L43277

Metabolisme

Niraparib is primarily metabolized by carboxylesterases (CEs) to form M1, which is a major inactive metabolite. The M1 metabolite can subsequently undergo glucuronidation mediated by UDP-glucuronosyltransferases (UGTs) to form the M10 metabolite.L43277 In a mass balance study, M1 and M10 were the major circulating metabolites.L43742 The M1 metabolite can also undergo methylation, monooxygenation, and hydrogenation to form other minor metabolites.A253937

Rute Eliminasi

Niraparib is eliminated via multiple pathways, including liver metabolism, hepatobiliary excretion, and renal elimination.L43747 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. In pooled samples collected over 6 days, unchanged niraparib accounted for 11% and 19% of the administered dose recovered in urine and feces, respectively.L43277

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food. Food does not affect the absorption of niraparib.

Interaksi Obat

38 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Niraparib.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Niraparib.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Niraparib.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Niraparib.
Lidocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Quinisocaine.
Ambroxol The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Niraparib is combined with Etrasimod.

Target Protein

Poly [ADP-ribose] polymerase 1 PARP1
Poly [ADP-ribose] polymerase 2 PARP2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21718592
    Chen A: PARP inhibitors: its role in treatment of cancer. Chin J Cancer. 2011 Jul;30(7):463-71. doi: 10.5732/cjc.011.10111.
  • PMID: 30073633
    Heo YA, Duggan ST: Niraparib: A Review in Ovarian Cancer. Target Oncol. 2018 Aug;13(4):533-539. doi: 10.1007/s11523-018-0582-1.
  • PMID: 29650751
    Ison G, Howie LJ, Amiri-Kordestani L, Zhang L, Tang S, Sridhara R, Pierre V, Charlab R, Ramamoorthy A, Song P, Li F, Yu J, Manheng W, Palmby TR, Ghosh S, Horne HN, Lee EY, Philip R, Dave K, Chen XH, Kelly SL, Janoria KG, Banerjee A, Eradiri O, Dinin J, Goldberg KB, Pierce WF, Ibrahim A, Kluetz PG, Blumenthal GM, Beaver JA, Pazdur R: FDA Approval Summary: Niraparib for the Maintenance Treatment of Patients with Recurrent Ovarian Cancer in Response to Platinum-Based Chemotherapy. Clin Cancer Res. 2018 Sep 1;24(17):4066-4071. doi: 10.1158/1078-0432.CCR-18-0042. Epub 2018 Apr 12.
  • PMID: 30069770
    Bochum S, Berger S, Martens UM: Olaparib. Recent Results Cancer Res. 2018;211:217-233. doi: 10.1007/978-3-319-91442-8_15.
  • PMID: 28303528
    van Andel L, Zhang Z, Lu S, Kansra V, Agarwal S, Hughes L, Tibben MM, Gebretensae A, Lucas L, Hillebrand MJX, Rosing H, Schellens JHM, Beijnen JH: Human mass balance study and metabolite profiling of (14)C-niraparib, a novel poly(ADP-Ribose) polymerase (PARP)-1 and PARP-2 inhibitor, in patients with advanced cancer. Invest New Drugs. 2017 Dec;35(6):751-765. doi: 10.1007/s10637-017-0451-2. Epub 2017 Mar 16.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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