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Identification
NameNetupitant
Accession NumberDB09048
TypeSmall Molecule
GroupsApproved
Description

Netupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy. Netupitant is a neurokinin 1 receptor antagonist. The combination drug is marketed by Eisai Inc. and Helsinn Therapeutics (U.S.) Inc. under the brand Akynzeo®.

Structure
Thumb
Synonyms
2-[3,5-Bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]propanamide
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
AkynzeoEisai Inc.
SaltsNot Available
Categories
UNII7732P08TIR
CAS number290297-26-6
WeightAverage: 578.603
Monoisotopic: 578.248030644
Chemical FormulaC30H32F6N4O
InChI KeyWAXQNWCZJDTGBU-UHFFFAOYSA-N
InChI
InChI=1S/C30H32F6N4O/c1-19-8-6-7-9-23(19)24-17-26(40-12-10-38(4)11-13-40)37-18-25(24)39(5)27(41)28(2,3)20-14-21(29(31,32)33)16-22(15-20)30(34,35)36/h6-9,14-18H,10-13H2,1-5H3
IUPAC Name
2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide
SMILES
CN(C(=O)C(C)(C)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CN=C(C=C1C1=CC=CC=C1C)N1CCN(C)CC1
Taxonomy
ClassificationNot classified
Pharmacology
IndicationNetupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy.
PharmacodynamicsNot Available
Mechanism of actionDelayed emesis (vomiting) has been largely associated with the activation of tachykinin family neurokinin 1 (NK1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.
Related Articles
AbsorptionUpon oral administration of a single dose of netupitant, netupitant started to be measurable in plasma between 15 minutes and 3 hours after dosing. Plasma concentrations reached Cmax in approximately 5 hours. There was a greater than dose-proportional increase in the systemic exposure with the dose increase from 10 mg to 300 mg and a dose-proportional increase in systemic exposure with a dose increase from 300 mg to 450 mg.
Volume of distribution

In cancer patients, Vz/F: 1982 ± 906 L (mean ± SD).

Protein binding> 99.5% at drug concentrations ranging from 10-1300 ng/mL.
Metabolism

Once absorbed, netupitant is extensively metabolized to form three major metabolites: desmethyl derivative, M1; N-oxide derivative, M2; and OH-methyl derivative, M3. Metabolism is mediated primarily by CYP3A4 and to a lesser extent by CYP2C9 and CYP2D6. Metabolites M1, M2 and M3 were shown to bind to the substance P/neurokinin 1 (NK1) receptor.

SubstrateEnzymesProduct
Netupitant
Desmethyl NetupitantDetails
Netupitant
N-oxide NetupitantDetails
Route of eliminationPrimarily fecal.
Half life96 hours with CV% of 61.
Clearance

estimated systemic clearance of 20.3 ± 9.2 L/h (mean ± SD).

ToxicityDaily oral administration of netupitant in rats at doses up to 30 mg/kg (1.9 times the human AUC in male rats and 3.7 times the human AUC in female rats at the recommended human dose) had no effects on fertility or reproductive performance.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6297375 No2000-02-222020-02-22Us
US8623826 No2010-11-182030-11-18Us
US8951969 No2010-11-182030-11-18Us
US9186357 No2010-11-182030-11-18Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00285 mg/mLALOGPS
logP5.48ALOGPS
logP7.26ChemAxon
logS-5.3ALOGPS
pKa (Strongest Basic)7.6ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area39.68 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity148.59 m3·mol-1ChemAxon
Polarizability55.88 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Darmani NA, Zhong W, Chebolu S, Mercadante F: Differential and additive suppressive effects of 5-HT3 (palonosetron)- and NK1 (netupitant)-receptor antagonists on cisplatin-induced vomiting and ERK1/2, PKA and PKC activation. Pharmacol Biochem Behav. 2015 Apr;131:104-11. doi: 10.1016/j.pbb.2015.02.010. Epub 2015 Feb 14. [PubMed:25687374 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (273 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Netupitant.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Netupitant.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Netupitant.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Netupitant.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Netupitant.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Netupitant.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Netupitant.
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Netupitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Netupitant.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Netupitant.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Netupitant.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Netupitant.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Netupitant.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Netupitant.
BexaroteneThe serum concentration of Netupitant can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Netupitant.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Netupitant.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Netupitant.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Netupitant.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Netupitant.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Netupitant.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Netupitant.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Netupitant.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Netupitant.
CarbamazepineThe serum concentration of Netupitant can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Netupitant.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Netupitant.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Netupitant.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Netupitant.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Netupitant.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Netupitant.
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Netupitant.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Netupitant.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Netupitant.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Netupitant.
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Netupitant.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Netupitant.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Netupitant.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Netupitant.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Netupitant.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Netupitant.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Netupitant.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Netupitant.
DarunavirThe serum concentration of Darunavir can be increased when it is combined with Netupitant.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Netupitant.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Netupitant.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Netupitant.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Netupitant.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Netupitant.
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Netupitant.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Netupitant.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Netupitant.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Netupitant.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Netupitant.
EnzalutamideThe serum concentration of Netupitant can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Netupitant.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Netupitant.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Netupitant.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Netupitant.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Netupitant.
EscitalopramThe serum concentration of Escitalopram can be increased when it is combined with Netupitant.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Netupitant.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Netupitant.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Netupitant.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Netupitant.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Netupitant.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Netupitant.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Netupitant.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Netupitant.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Netupitant.
FluvoxamineNetupitant may increase the serotonergic activities of Fluvoxamine.
FosaprepitantThe serum concentration of Fosaprepitant can be increased when it is combined with Netupitant.
FosphenytoinThe serum concentration of Netupitant can be decreased when it is combined with Fosphenytoin.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Netupitant.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Netupitant.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Netupitant.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Netupitant.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Netupitant.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Netupitant.
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Netupitant.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Netupitant.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Netupitant.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Netupitant.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Netupitant.
ItraconazoleThe serum concentration of Itraconazole can be increased when it is combined with Netupitant.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Netupitant.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Netupitant.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Netupitant.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Netupitant.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Netupitant.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Netupitant.
MacitentanThe serum concentration of MACITENTAN can be increased when it is combined with Netupitant.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Netupitant.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Netupitant.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Netupitant.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Netupitant.
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Netupitant.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Netupitant.
MitotaneThe serum concentration of Netupitant can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Netupitant.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Netupitant.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Netupitant.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Netupitant.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Netupitant.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Netupitant.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Netupitant.
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Netupitant.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Netupitant.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Netupitant.
PhenobarbitalThe serum concentration of Netupitant can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Netupitant can be decreased when it is combined with Phenytoin.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Netupitant.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Netupitant.
PrimidoneThe serum concentration of Netupitant can be decreased when it is combined with Primidone.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Netupitant.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Netupitant.
QuinineThe serum concentration of Quinine can be increased when it is combined with Netupitant.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Netupitant.
RifabutinThe serum concentration of Netupitant can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Netupitant can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Netupitant can be decreased when it is combined with Rifapentine.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Netupitant.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Netupitant.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Netupitant.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Netupitant.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Netupitant.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Netupitant.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Netupitant.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Netupitant.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Netupitant.
St. John's WortThe serum concentration of Netupitant can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Netupitant.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Netupitant.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Netupitant.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Netupitant.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Netupitant.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Netupitant.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Netupitant.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Netupitant.
TelithromycinThe serum concentration of Telithromycin can be increased when it is combined with Netupitant.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Netupitant.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Netupitant.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Netupitant.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Netupitant.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Netupitant.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Netupitant.
TramadolNetupitant may increase the serotonergic activities of Tramadol.
Trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Netupitant.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Netupitant.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Netupitant.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Netupitant.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Netupitant.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Netupitant.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Netupitant.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Netupitant.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Netupitant.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Netupitant.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Netupitant.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Netupitant.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Netupitant.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Tachykinin receptor activity
Specific Function:
This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K.
Gene Name:
TACR1
Uniprot ID:
P25103
Molecular Weight:
46250.5 Da
References
  1. Darmani NA, Zhong W, Chebolu S, Mercadante F: Differential and additive suppressive effects of 5-HT3 (palonosetron)- and NK1 (netupitant)-receptor antagonists on cisplatin-induced vomiting and ERK1/2, PKA and PKC activation. Pharmacol Biochem Behav. 2015 Apr;131:104-11. doi: 10.1016/j.pbb.2015.02.010. Epub 2015 Feb 14. [PubMed:25687374 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
substrate
General Function:
Monooxygenase activity
Specific Function:
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name:
CYP3A43
Uniprot ID:
Q9HB55
Molecular Weight:
57669.21 Da
References
  1. Calcagnile S, Lanzarotti C, Rossi G, Henriksson A, Kammerer KP, Timmer W: Effect of netupitant, a highly selective NK(1) receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Support Care Cancer. 2013 Oct;21(10):2879-87. doi: 10.1007/s00520-013-1857-9. Epub 2013 Jun 11. [PubMed:23748441 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
substrate
General Function:
Steroid hydroxylase activity
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Calcagnile S, Lanzarotti C, Rossi G, Henriksson A, Kammerer KP, Timmer W: Effect of netupitant, a highly selective NK(1) receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Support Care Cancer. 2013 Oct;21(10):2879-87. doi: 10.1007/s00520-013-1857-9. Epub 2013 Jun 11. [PubMed:23748441 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Calcagnile S, Lanzarotti C, Rossi G, Henriksson A, Kammerer KP, Timmer W: Effect of netupitant, a highly selective NK(1) receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Support Care Cancer. 2013 Oct;21(10):2879-87. doi: 10.1007/s00520-013-1857-9. Epub 2013 Jun 11. [PubMed:23748441 ]
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Drug created on May 04, 2015 10:50 / Updated on June 26, 2016 01:53