Niraparib
Identification
- Summary
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.
- Brand Names
- Zejula
- Generic Name
- Niraparib
- DrugBank Accession Number
- DB11793
- Background
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.6 Niraparib is selective towards PARP-1 and PARP-2.2 First approved by the FDA on March 27, 2017,3 niraparib is used to treat epithelial ovarian, fallopian tube, or primary peritoneal cancer.6 Niraparib was approved by the European Commission on November 16, 2017 7 and by Health Canada on June 27, 2019.8
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 320.396
Monoisotopic: 320.16371128 - Chemical Formula
- C19H20N4O
- Synonyms
- Niraparib
- External IDs
- MK 4827
- MK-4827
- MK-4827 FREE BASE
- MK4827
Pharmacology
- Indication
Niraparib is indicated for the maintenance treatment of adult patients with advanced or recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy.6,7,8
In Canada and the US, niraparib is also available in a combination product with abiraterone, which is indicated with prednisone for the treatment of adults with deleterious or suspected deleterious BRCA-mutated (BRCAm) metastatic castration-resistant prostate cancer (mCRPC).9,10 In Canada, this combination product is also used with prednisolone and is reserved for patients who are asymptomatic or mildly symptomatic, and in whom chemotherapy is not clinically indicated.9
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Advanced epithelial ovarian cancer •••••••••••• ••••• •••••••••• •• •••••••••••••• •••••••••••• Treatment of Advanced primary peritoneal carcinoma •••••••••••• ••••• •••••••••• •• •••••••••••••• •••••••••••• Used in combination to treat Metastatic castration-resistant prostate cancer (mcrpc) Regimen in combination with: Prednisone (DB00635), Abiraterone (DB05812) •••••••••••• ••••• •••••• Used in combination to treat Metastatic castration-resistant prostate cancer (mcrpc) Combination Product in combination with: Abiraterone (DB05812) •••••••••••• ••••• ••••••••••••• •••••••••••• ••• •••••••••• ••••••••• •••••• Used in combination to treat Metastatic castration-resistant prostate cancer (mcrpc) Combination Product in combination with: Abiraterone (DB05812) •••••••••••• ••••• •••• •••••••• ••••••••• •••••••••••• ••• •••••••••• ••••••••• •••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Niraparib mediated cytotoxic effects in tumour cell lines with or without deficiencies in BRCA1/2. Decreased tumour growth was observed in both mouse xenograft models of human cancer cell lines with deficiencies in BRCA1/2 and human patient-derived xenograft tumour models with homologous recombination deficiency (HRD) that had either mutated or wild-type BRCA1/2.6
In vitro studies suggest that niraparib inhibits dopamine, norepinephrine, and serotonin transporters, which may explain its off-target cardiovascular effects such as increased pulse rate and blood pressure.2
- Mechanism of action
Niraparib is a potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes, PARP-1 and PARP-2.7,8 PARPs play an important role in DNA repair. They recognize and repair cellular DNA damage, such as single-strand breaks (SSBs) and double-strand breaks (DSBs). Different DNA repair pathways exist to repair these DNA damages, including the base excision repair (BER) pathway for SSBs and BRCA-dependent homologous recombination for DSBs.4 If BER is impaired, SSBs accumulate and become DSBs, forcing cells to rely on other repair pathways, mainly the homologous recombination (HR) and the nonhomologous end joining, to repair DNA damages.1 However, some cells can have defective or deficient HR resulting from specific mutations in DNA repair genes, such as BRCA1 and 2.2 Inhibiting PARPs in the presence of HR deficiency leads to a phenomenon called 'synthetic lethality,' whereby the PARP inhibitor impedes BER, leading to genetic instability and cell death.1,2
Selectivity towards PARP-1 and PARP-2 is 100-fold higher than for other PARP family members.2 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.6,7,8
Target Actions Organism APoly [ADP-ribose] polymerase 1 inhibitorHumans APoly [ADP-ribose] polymerase 2 inhibitorHumans - Absorption
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.6
The absolute bioavailability of niraparib is approximately 73%. Food does not appear to affect drug exposure.6
- Volume of distribution
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.6
- Protein binding
Niraparib is 83% bound to human plasma proteins.6
- Metabolism
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.6 In a mass balance study, M1 and M10 were the major circulating metabolites.7 The M1 metabolite can also undergo methylation, monooxygenation, and hydrogenation to form other minor metabolites.5
Hover over products below to view reaction partners
- Route of elimination
Niraparib is eliminated via multiple pathways, including liver metabolism, hepatobiliary excretion, and renal elimination.8 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.6
- Half-life
Following multiple daily doses of 300 mg of niraparib, the mean half-life (t1/2) is 36 hours.6
- Clearance
In a population pharmacokinetic analysis, the apparent total clearance (CL/F) of niraparib was 16.2 L/h in patients with cancer.6
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There is limited information available regarding the acute toxicity profile and overdosage of niraparib.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAmbroxol The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Ambroxol. Articaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Benzyl alcohol. Bupivacaine The risk or severity of methemoglobinemia can be increased when Niraparib is combined with Bupivacaine. - Food Interactions
- Take at the same time every day.
- Take with or without food. Food does not affect the absorption of niraparib.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Niraparib hydrochloride L4JFC1PHCI 1038915-64-8 YXYDNYFWAFBCAN-PFEQFJNWSA-N Niraparib tosylate 75KE12AY9U 1038915-73-9 LCPFHXWLJMNKNC-PFEQFJNWSA-N Niraparib tosylate monohydrate 195Q483UZD 1613220-15-7 ACNPUCQQZDAPJH-FMOMHUKBSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Zejula Tablet, film coated 100 mg Oral Glaxo Smith Kline (Ireland) Limited 2023-11-14 Not applicable EU Zejula Capsule 100 mg Oral Glaxo Smith Kline (Ireland) Limited 2020-12-16 Not applicable EU Zejula Tablet, film coated 200 mg/1 Oral GlaxoSmithKline LLC 2023-06-27 Not applicable US Zejula Capsule 100 mg Oral Glaxosmithkline Inc 2020-01-09 Not applicable Canada Zejula Tablet, film coated 100 mg Oral Glaxo Smith Kline (Ireland) Limited 2023-11-14 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Akeega Niraparib (50 mg) + Abiraterone acetate (500 mg) Tablet, film coated Oral Janssen Cilag International Nv 2023-06-09 Not applicable EU Akeega Niraparib tosylate (100 mg) + Abiraterone acetate (500 mg) Tablet Oral Janssen Pharmaceuticals 2023-08-14 Not applicable Canada Akeega Niraparib tosylate monohydrate (50 mg/1) + Abiraterone acetate (500 mg/1) Tablet, film coated Oral Janssen Biotech, Inc. 2023-08-11 Not applicable US Akeega Niraparib tosylate (50 mg) + Abiraterone acetate (500 mg) Tablet Oral Janssen Pharmaceuticals 2023-08-14 Not applicable Canada Akeega Niraparib (100 mg) + Abiraterone acetate (500 mg) Tablet, film coated Oral Janssen Cilag International Nv 2023-06-09 Not applicable EU
Categories
- ATC Codes
- L01XK02 — Niraparib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (weak)
- Cytochrome P-450 Enzyme Inducers
- Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- MATE 1 Inhibitors
- MATE 1 Substrates
- MATE 1 Substrates with a Narrow Therapeutic Index
- MATE 2 Inhibitors
- MATE 2 Substrates
- MATE 2 Substrates with a Narrow Therapeutic Index
- MATE inhibitors
- MATE substrates
- Narrow Therapeutic Index Drugs
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Poly (ADP-ribose) polymerase (PARP) inhibitors
- Poly(ADP-ribose) Polymerase Inhibitors
- Pyrazoles
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Piperidines
- Sub Class
- Phenylpiperidines
- Direct Parent
- Phenylpiperidines
- Alternative Parents
- Phenylpyrazoles / Indazoles / Aralkylamines / Benzene and substituted derivatives / Heteroaromatic compounds / Primary carboxylic acid amides / Amino acids and derivatives / Dialkylamines / Azacyclic compounds / Organooxygen compounds show 2 more
- Substituents
- Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Benzopyrazole / Carboxamide group / Carboxylic acid derivative show 15 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- HMC2H89N35
- CAS number
- 1038915-60-4
- InChI Key
- PCHKPVIQAHNQLW-CQSZACIVSA-N
- InChI
- InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
- IUPAC Name
- 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
- SMILES
- NC(=O)C1=CC=CC2=CN(N=C12)C1=CC=C(C=C1)[C@@H]1CCCNC1
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Bochum S, Berger S, Martens UM: Olaparib. Recent Results Cancer Res. 2018;211:217-233. doi: 10.1007/978-3-319-91442-8_15. [Article]
- 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. [Article]
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- EMA Approved Drug Products: Zejula (niraparib) Oral Capsules [Link]
- Health Canada Approved Drug Products: ZEJULA (niraparib) Oral Capsules or Tablets [Link]
- Health Canada Approved Drug Proucts: AKEEGA (Niraparib and abiraterone acetate) tablets for oral use [Link]
- FDA Approved Drug Products: AKEEGA (niraparib and abiraterone acetate) tablets, for oral use [Link]
- External Links
- PubChem Compound
- 24958200
- PubChem Substance
- 347828142
- ChemSpider
- 24531930
- BindingDB
- 50316226
- 1918231
- ChEBI
- 176844
- ChEMBL
- CHEMBL1094636
- ZINC
- ZINC000043206370
- PharmGKB
- PA166131610
- PDBe Ligand
- 3JD
- Wikipedia
- Niraparib
- PDB Entries
- 4r6e / 7f43 / 7kk5 / 7kkp / 8i2m
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Ovarian Cancer 1 4 Not Yet Recruiting Treatment Epithelial Ovarian Cancer / Ovarian Cancer / Stage III Ovarian Cancer / Stage IV Ovarian Cancer 1 4 Recruiting Prevention Adult Patients With Platinum-sensitive, Relapsed, High Grade Serous Epithelial Ovarian Cancer 1 3 Active Not Recruiting Treatment Breast Neoplasms 1 3 Active Not Recruiting Treatment Castration Resistant Prostate Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet, film coated Oral Capsule Oral 100 mg Capsule Oral 100 mg/1 Tablet Oral 100 mg Tablet, film coated Oral 100 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 200 mg/1 Tablet, film coated Oral 300 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8859562 No 2014-10-14 2031-08-04 US US8143241 No 2012-03-27 2027-08-12 US US8071579 No 2011-12-06 2027-08-12 US US8071623 No 2011-12-06 2030-03-22 US US8436185 No 2013-05-07 2029-04-24 US US11091459 No 2021-08-17 2038-03-27 US US11673877 No 2018-03-27 2038-03-27 US US11207311 No 2021-12-28 2037-07-28 US US11730725 No 2019-01-04 2039-01-04 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 463 https://file.medchemexpress.com/batch_PDF/HY-10619/Niraparib-SDS-MedChemExpress.pdf - Predicted Properties
Property Value Source Water Solubility 0.0149 mg/mL ALOGPS logP 2.45 ALOGPS logP 2.47 Chemaxon logS -4.3 ALOGPS pKa (Strongest Acidic) 14.03 Chemaxon pKa (Strongest Basic) 10.08 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 72.94 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 94.92 m3·mol-1 Chemaxon Polarizability 36.4 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0fk9-0009000000-0c70995be19b18915530 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-0019000000-1388e4a12d215f990898 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0udi-0009000000-5c85ca7c860bb4d24ba6 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0ukd-0896000000-f65ad9bda964f9894915 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0019000000-eeb821d574d7bde1221c Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00kf-2592000000-8fb7f4c5972faed3a84c Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 197.5784799 predictedDarkChem Lite v0.1.0 [M-H]- 174.91042 predictedDeepCCS 1.0 (2019) [M+H]+ 197.2974799 predictedDarkChem Lite v0.1.0 [M+H]+ 177.44865 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.3550799 predictedDarkChem Lite v0.1.0 [M+Na]+ 184.7957 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP1
- Uniprot ID
- P09874
- Uniprot Name
- Poly [ADP-ribose] polymerase 1
- Molecular Weight
- 113082.945 Da
References
- 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. [Article]
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- EMA Approved Drug Products: Zejula (niraparib) Oral Capsules [Link]
- Health Canada Approved Drug Products: ZEJULA (niraparib) Oral Capsules or Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Nad+ adp-ribosyltransferase activity
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP2
- Uniprot ID
- Q9UGN5
- Uniprot Name
- Poly [ADP-ribose] polymerase 2
- Molecular Weight
- 66205.31 Da
References
- 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. [Article]
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- EMA Approved Drug Products: Zejula (niraparib) Oral Capsules [Link]
- Health Canada Approved Drug Products: ZEJULA (niraparib) Oral Capsules or Tablets [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Carboxylic ester hydrolase activity
- Specific Function
- Not Available
- Gene Name
- CES1A1a
- Uniprot ID
- Q6LAP9
- Uniprot Name
- Carboxylesterase
- Molecular Weight
- 1908.25 Da
References
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- Curator comments
- Niraparib weakly induces CYP1A2 in vitro.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Health Canada Approved Drug Products: ZEJULA (niraparib) Oral Capsules or Tablets [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- Curator comments
- Niraparib inhibits MATE1 with IC50 of 0.18 microM. Niraparib M1 metabolite is a substrate of MATE1.
- General Function
- Monovalent cation:proton antiporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
- Gene Name
- SLC47A1
- Uniprot ID
- Q96FL8
- Uniprot Name
- Multidrug and toxin extrusion protein 1
- Molecular Weight
- 61921.585 Da
References
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- Curator comments
- Niraparib inhibits MATE2 with IC50 of ≤0.14 microM. Niraparib M1 metabolite is a substrate of MATE2.
- General Function
- Drug transmembrane transporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
- Gene Name
- SLC47A2
- Uniprot ID
- Q86VL8
- Uniprot Name
- Multidrug and toxin extrusion protein 2
- Molecular Weight
- 65083.915 Da
References
- FDA Approved Drug Products: ZEJULA (niraparib) capsules, for oral use (September 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
Drug created at October 20, 2016 20:48 / Updated at February 20, 2024 23:54