You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameVemurafenib
Accession NumberDB08881
TypeSmall Molecule
GroupsApproved
Description

Vemurafenib is a BRAF enzyme inhibitor developed by Plexxikon and Genentech for the treatment of late-stage melanoma. [Wikipedia] The cobas® 4800 BRAF B600 mutation test provided by Roche Molecular Systems is the diagnostic test to confirm eligibility for treatment. FDA approved on August 17, 2011 under the company Hoffmann La Roche.

Structure
Thumb
Synonyms
BRAF(V600E) Kinase Inhibitor RO5185426
PLX4032
Zelboraf
External Identifiers
  • RG7204
  • RO5185426
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zelboraftablet, film coated240 mg/1oralGenentech, Inc.2011-08-17Not applicableUs
Zelboraftablet240 mgoralHoffmann La Roche Limited2012-03-05Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII207SMY3FQT
CAS number918504-65-1
WeightAverage: 489.922
Monoisotopic: 489.072546264
Chemical FormulaC23H18ClF2N3O3S
InChI KeyInChIKey=GPXBXXGIAQBQNI-UHFFFAOYSA-N
InChI
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
IUPAC Name
N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide
SMILES
CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=NC=C(C=C23)C2=CC=C(Cl)C=C2)=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassPhenylpyridines
Direct ParentPhenylpyridines
Alternative Parents
Substituents
  • 3-phenylpyridine
  • Sulfanilide
  • Pyrrolopyridine
  • Acetophenone
  • Aryl ketone
  • Benzoyl
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Benzenoid
  • Substituted pyrrole
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Vinylogous amide
  • Vinylogous halide
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Pyrrole
  • Ketone
  • Azacycle
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
PharmacodynamicsNot Available
Mechanism of actionVemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
Related Articles
AbsorptionAfter oral administration of vemurafenib, it is well absorbed. Bioavailability is unknown. Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. Exposure is highly variable between different patients. Gastrointestinal fluid content, pH, volumes, motility, transition time and bile composition may be factors affecting exposure. It is unknown how food affects the absorption of vemurafenib. Time to steady state = 15 - 22 days
Volume of distribution

106 L

Protein binding>99% protein bound to serum albumin and alpha-1 acid glycoprotein.
Metabolism

Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.

Route of eliminationExcreted via feces (94%) and urine (1%).
Half lifeElimination half-life = 57 hours (range of 30-120 hours)
Clearance

Total body clearance = 31 L/day

ToxicityNot Available
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 Absorption+1.0
Blood Brain Barrier+0.745
Caco-2 permeable-0.6222
P-glycoprotein substrateNon-substrate0.6215
P-glycoprotein inhibitor INon-inhibitor0.5884
P-glycoprotein inhibitor IINon-inhibitor0.699
Renal organic cation transporterNon-inhibitor0.864
CYP450 2C9 substrateNon-substrate0.7628
CYP450 2D6 substrateNon-substrate0.8038
CYP450 3A4 substrateSubstrate0.5645
CYP450 1A2 substrateInhibitor0.5762
CYP450 2C9 inhibitorInhibitor0.5987
CYP450 2D6 inhibitorNon-inhibitor0.7329
CYP450 2C19 inhibitorInhibitor0.6508
CYP450 3A4 inhibitorInhibitor0.7061
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9553
Ames testNon AMES toxic0.6323
CarcinogenicityNon-carcinogens0.7229
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5179 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6688
hERG inhibition (predictor II)Non-inhibitor0.5302
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral240 mg
Tablet, film coatedoral240 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7504509 No2006-10-222026-10-22Us
US7863288 No2009-06-202029-06-20Us
US8143271 No2006-06-212026-06-21Us
US8470818 No2006-08-022026-08-02Us
US8741920 No2010-07-272030-07-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point272°CMSDS
water solubility<1 mg/mL MSDS
logP5.1MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.000362 mg/mLALOGPS
logP4.95ALOGPS
logP4.62ChemAxon
logS-6.1ALOGPS
pKa (Strongest Acidic)7.17ChemAxon
pKa (Strongest Basic)3.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area91.92 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity121.97 m3·mol-1ChemAxon
Polarizability48.1 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
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. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
External Links
ATC CodesL01XE15
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (304 KB)
MSDSDownload (51 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Vemurafenib.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Vemurafenib.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Vemurafenib.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.
AprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Vemurafenib.
AtazanavirThe serum concentration of Vemurafenib can be increased when it is combined with Atazanavir.
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Vemurafenib.
BexaroteneThe serum concentration of Vemurafenib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Vemurafenib can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Vemurafenib.
BosentanThe serum concentration of Vemurafenib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Vemurafenib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Vemurafenib.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Vemurafenib.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Vemurafenib.
CarbamazepineThe serum concentration of Vemurafenib can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Vemurafenib can be increased when it is combined with Ceritinib.
CitalopramCitalopram may increase the QTc-prolonging activities of Vemurafenib.
ClarithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Clarithromycin.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Vemurafenib.
CobicistatThe serum concentration of Vemurafenib can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Vemurafenib.
ConivaptanThe serum concentration of Vemurafenib can be increased when it is combined with Conivaptan.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Vemurafenib.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Vemurafenib.
DabrafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Dabrafenib.
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Vemurafenib.
DarunavirThe serum concentration of Vemurafenib can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Vemurafenib can be decreased when it is combined with Deferasirox.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Vemurafenib.
DofetilideDofetilide may increase the QTc-prolonging activities of Vemurafenib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Vemurafenib.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Vemurafenib.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Vemurafenib.
EnzalutamideThe serum concentration of Vemurafenib can be decreased when it is combined with Enzalutamide.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Vemurafenib.
FluconazoleThe metabolism of Vemurafenib can be decreased when combined with Fluconazole.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Vemurafenib.
FluvoxamineThe serum concentration of Fluvoxamine can be increased when it is combined with Vemurafenib.
FosaprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Vemurafenib can be increased when it is combined with Fusidic Acid.
GoserelinGoserelin may increase the QTc-prolonging activities of Vemurafenib.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Vemurafenib.
IdelalisibThe serum concentration of Vemurafenib can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Vemurafenib can be increased when it is combined with Indinavir.
IpilimumabIpilimumab may increase the hepatotoxic activities of Vemurafenib.
ItraconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Vemurafenib.
IvacaftorThe serum concentration of Vemurafenib can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Ketoconazole.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Vemurafenib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Vemurafenib.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Vemurafenib.
LuliconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Luliconazole.
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.
MifepristoneMifepristone may increase the QTc-prolonging activities of Vemurafenib.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Vemurafenib.
MitotaneThe serum concentration of Vemurafenib can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Vemurafenib.
NefazodoneThe serum concentration of Vemurafenib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Vemurafenib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Vemurafenib can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Vemurafenib.
OctreotideOctreotide may increase the QTc-prolonging activities of Vemurafenib.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Vemurafenib.
PalbociclibThe serum concentration of Vemurafenib can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.
PhenobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Phenytoin.
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Vemurafenib.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Vemurafenib.
PorfimerVemurafenib may increase the photosensitizing activities of Porfimer.
PosaconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Vemurafenib can be decreased when it is combined with Primidone.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Vemurafenib.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Vemurafenib.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Vemurafenib.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Vemurafenib.
RifabutinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Vemurafenib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Vemurafenib.
RitonavirThe serum concentration of Vemurafenib can be increased when it is combined with Ritonavir.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Vemurafenib.
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Vemurafenib.
SaquinavirThe serum concentration of Vemurafenib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Vemurafenib.
SiltuximabThe serum concentration of Vemurafenib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Vemurafenib can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Vemurafenib can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Vemurafenib can be increased when it is combined with Stiripentol.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Vemurafenib.
TelaprevirThe serum concentration of Vemurafenib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Telithromycin.
TesmilifeneThe serum concentration of Vemurafenib can be decreased when it is combined with Tesmilifene.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Vemurafenib.
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Vemurafenib.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
TocilizumabThe serum concentration of Vemurafenib can be decreased when it is combined with Tocilizumab.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Vemurafenib.
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Vemurafenib.
VerapamilThe serum concentration of Vemurafenib can be increased when it is combined with Verapamil.
VerteporfinVemurafenib may increase the photosensitizing activities of Verteporfin.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Vemurafenib.
VoriconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Vemurafenib.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, and thereby contributes to the MAP kinase signal transduction pathway.
Gene Name:
BRAF
Uniprot ID:
P15056
Molecular Weight:
84436.135 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Vitamin d3 25-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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF: Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032). J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27. [PubMed:22454535 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF: Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032). J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27. [PubMed:22454535 ]
Comments
comments powered by Disqus
Drug created on May 20, 2013 00:41 / Updated on June 30, 2016 01:52