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Identification
NameEtravirine
Accession NumberDB06414
TypeSmall Molecule
GroupsApproved
Description

Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor(NNRTI). Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection.
On January 18, 2007, the FDA granted accelerated approved for the use of etravirine 100mg tablets in the treatment of adult HIV-1 infection documented to be resistant to therapy with other NNRTIs and antiretroviral agents. On March 26, 2012, approval was extended for use in treatment-experienced pediatric patients 6 to 18 years of age, weighing at least 16 kg. Etravarine must always be used in combination with other antiretroviral drugs.

Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1), and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.

Common side effects of use include mild to moderate rash within the first 6 weeks of therapy, nausea, diarrhea and peripheral neuropathy. Patients are advised to immediately contact their healthcare provider if a rash develops.

In 2009, postmarketing case reports of Stevens-Johnson Syndrome, toxic epidermal necrolysis, erythema multiforme, and other hypersensitivity reactions lead to a revision of etravirine’s “Warnings and Precautions,” as well as notification of health care providers.

In 2013, reports of Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré
syndrome) in the setting of immune reconstitution, as well as more in depth information about the development of rashes in patients taking etravirine, lead to a modification of etravirine’s monograph.

Structure
Thumb
Synonyms
Intelence
External Identifiers
  • R165335
  • TMC125
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Intelencetablet200 mgoralJanssen Inc2011-12-12Not applicableCanada
Intelencetablet100 mg/1oralREMEDYREPACK INC.2013-03-182016-04-05Us
Intelencetablet100 mgoralJanssen Inc2008-03-27Not applicableCanada
Intelencetablet25 mg/1oralJanssen Products LP2012-03-26Not applicableUs
Intelencetablet200 mg/1oralJanssen Products LP2010-12-22Not applicableUs
Intelencetablet100 mg/1oralJanssen Products LP2008-01-18Not applicableUs
Intelencetablet200 mg/1oralPhysicians Total Care, Inc.2012-10-10Not applicableUs
Intelencetablet100 mg/1oralPhysicians Total Care, Inc.2008-02-21Not applicableUs
Intelencetablet25 mgoralJanssen Inc2013-06-14Not applicableCanada
Intelencetablet100 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
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
UNII0C50HW4FO1
CAS number269055-15-4
WeightAverage: 435.277
Monoisotopic: 434.049071779
Chemical FormulaC20H15BrN6O
InChI KeyInChIKey=PYGWGZALEOIKDF-UHFFFAOYSA-N
InChI
InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27)
IUPAC Name
4-({6-amino-5-bromo-2-[(4-cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-dimethylbenzonitrile
SMILES
CC1=CC(=CC(C)=C1OC1=C(Br)C(N)=NC(NC2=CC=C(C=C2)C#N)=N1)C#N
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassEthers
Sub ClassDiarylethers
Direct ParentDiarylethers
Alternative Parents
Substituents
  • Diaryl ether
  • Benzonitrile
  • Halopyrimidine
  • Aminopyrimidine
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Primary aromatic amine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl bromide
  • Heteroaromatic compound
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Nitrile
  • Carbonitrile
  • Hydrocarbon derivative
  • Primary amine
  • Organonitrogen compound
  • Organobromide
  • Organohalogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationIndicated as an adjunct therapy in the treatment of adult HIV-1 infections resistant to therapy with other NNRTIs and antiretroviral agents.
PharmacodynamicsClinical trials have shown no prolongation of QT intervals on electrocardiograms after 8 days of dosing.
Mechanism of actionEtravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.
Related Articles
AbsorptionMaximum oral absorption is achieved in 2.5-4 hours. Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity. Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal.
Volume of distribution

Distribution of etravirine into compartments other than plasma has not been evaluated in humans.

Protein bindingPlasma protein binding is about 99.9% in vitro. In vitro, 99.6% is bound to albumin, and 97.66% - 99.02% is bound to 1-alpha glycoprotein.
Metabolism

Metabolized (in vitro) by the liver CYP450 enzymes: CYP3A4, CYP2C9, CYP2C19. The major metabolites formed by a methyl hydroxylation of the dimethylbenzonitrile moiety retained less than 90% of etravirine's activity.

Route of eliminationAfter a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed. Etravirine is dialyzable (hemodialysis).
Half lifeHalf life of 9.05-41 hours.
Clearance

Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment.

Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments.

ToxicityNot Available
Affected organismsNot Available
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
Tabletoral100 mg/1
Tabletoral100 mg
Tabletoral200 mg/1
Tabletoral200 mg
Tabletoral25 mg/1
Tabletoral25 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2350801 No2008-05-202019-09-24Canada
CA2651665 No2010-04-272027-06-06Canada
US6878717 No1999-11-052019-11-05Us
US7037917 No2000-12-132020-12-13Us
US7887845 No1999-03-252019-03-25Us
US8003789 No1999-11-012019-11-01Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0169 mg/mLALOGPS
logP3.67ALOGPS
logP5.54ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)12.49ChemAxon
pKa (Strongest Basic)4.13ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area120.64 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity111.87 m3·mol-1ChemAxon
Polarizability41.09 Å3ChemAxon
Number of Rings3ChemAxon
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. Food and Drug Administration. [Internet] Janssen Pharmaceuticals; 2008 [Updated March 2012; cited Aug 2013].

2. Lexi-Comp, Inc. (Lexi-DrugsTM ). Lexi-Comp, Inc.; July, 2013.

External Links
ATC CodesJ05AG04
AHFS CodesNot Available
PDB Entries
FDA labelDownload (642 KB)
MSDSDownload (122 KB)
Interactions
Drug Interactions
Drug
AmiodaroneThe serum concentration of Amiodarone can be decreased when it is combined with Etravirine.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Etravirine.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Etravirine resulting in a loss in efficacy.
AtazanavirThe serum concentration of Etravirine can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be decreased when it is combined with Etravirine.
AvanafilThe serum concentration of Avanafil can be decreased when it is combined with Etravirine.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Etravirine.
BatimastatThe serum concentration of Etravirine can be decreased when it is combined with Batimastat.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Etravirine.
BepridilThe serum concentration of Bepridil can be decreased when it is combined with Etravirine.
BexaroteneThe serum concentration of Etravirine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Etravirine can be decreased when it is combined with Boceprevir.
BortezomibThe metabolism of Bortezomib can be decreased when combined with Etravirine.
BosentanThe serum concentration of Etravirine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Etravirine.
BuprenorphineThe serum concentration of Buprenorphine can be decreased when it is combined with Etravirine.
CarbamazepineThe serum concentration of Etravirine can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Etravirine.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Etravirine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Etravirine.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Etravirine.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Etravirine resulting in a loss in efficacy.
DabrafenibThe serum concentration of Etravirine can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Etravirine.
DarunavirThe serum concentration of Etravirine can be decreased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Etravirine can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Etravirine can be decreased when it is combined with Delavirdine.
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Etravirine.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Etravirine.
DisopyramideThe serum concentration of Disopyramide can be decreased when it is combined with Etravirine.
DolutegravirThe serum concentration of Dolutegravir can be decreased when it is combined with Etravirine.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Etravirine.
EfavirenzThe serum concentration of Etravirine can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Etravirine.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Etravirine.
FlecainideThe serum concentration of Flecainide can be decreased when it is combined with Etravirine.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Etravirine.
FluconazoleThe serum concentration of Etravirine can be increased when it is combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be decreased when it is combined with Etravirine.
FluvastatinThe serum concentration of Fluvastatin can be decreased when it is combined with Etravirine.
FosamprenavirThe serum concentration of the active metabolites of Fosamprenavir can be increased when Fosamprenavir is used in combination with Etravirine.
FosphenytoinThe serum concentration of Etravirine can be decreased when it is combined with Fosphenytoin.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Etravirine.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Etravirine.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Etravirine resulting in a loss in efficacy.
IndinavirThe serum concentration of Etravirine can be decreased when it is combined with Indinavir.
IsoflurophateThe serum concentration of Etravirine can be decreased when it is combined with Isoflurophate.
ItraconazoleThe serum concentration of Etravirine can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Etravirine can be increased when it is combined with Ketoconazole.
LidocaineThe serum concentration of Lidocaine can be decreased when it is combined with Etravirine.
LovastatinThe serum concentration of Lovastatin can be decreased when it is combined with Etravirine.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Etravirine.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Etravirine.
MexiletineThe serum concentration of Mexiletine can be decreased when it is combined with Etravirine.
MitotaneThe serum concentration of Etravirine can be decreased when it is combined with Mitotane.
NelfinavirThe serum concentration of Etravirine can be decreased when it is combined with Nelfinavir.
NevirapineThe serum concentration of Etravirine can be decreased when it is combined with Nevirapine.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Etravirine.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Etravirine.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Etravirine.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Etravirine.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Etravirine.
PhenobarbitalThe serum concentration of Etravirine can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Etravirine can be decreased when it is combined with Phenytoin.
PosaconazoleThe serum concentration of Etravirine can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Etravirine can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Etravirine.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Etravirine.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Etravirine.
RifabutinThe serum concentration of Etravirine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Etravirine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Etravirine can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Etravirine.
RitonavirThe serum concentration of Etravirine can be decreased when it is combined with Ritonavir.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Etravirine.
SaquinavirThe serum concentration of Etravirine can be decreased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Etravirine.
SecobarbitalThe metabolism of Etravirine can be increased when combined with Secobarbital.
SildenafilThe serum concentration of Sildenafil can be decreased when it is combined with Etravirine.
SiltuximabThe serum concentration of Etravirine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Etravirine.
SimvastatinThe serum concentration of Simvastatin can be decreased when it is combined with Etravirine.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Etravirine.
St. John's WortThe serum concentration of Etravirine can be decreased when it is combined with St. John&#39;s Wort.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Etravirine.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Etravirine.
TipranavirThe serum concentration of Etravirine can be decreased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Etravirine can be decreased when it is combined with Tocilizumab.
VardenafilThe serum concentration of Vardenafil can be decreased when it is combined with Etravirine.
VoriconazoleThe serum concentration of Etravirine can be increased when it is combined with Voriconazole.
Food InteractionsNot Available

Enzymes

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. Perez VE, Sanchez-Parra C, Serrano Villar S: [Etravirine drug interactions]. Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:27-31. doi: 10.1016/S0213-005X(09)73216-1. [PubMed:20116625 ]
  2. Kakuda TN, Scholler-Gyure M, Hoetelmans RM: Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet. 2011 Jan;50(1):25-39. doi: 10.2165/11534740-000000000-00000. [PubMed:21142266 ]
  3. Scholler-Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM: Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. doi: 10.2165/10895940-000000000-00000. [PubMed:19725591 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Perez VE, Sanchez-Parra C, Serrano Villar S: [Etravirine drug interactions]. Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:27-31. doi: 10.1016/S0213-005X(09)73216-1. [PubMed:20116625 ]
  2. Kakuda TN, Scholler-Gyure M, Hoetelmans RM: Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet. 2011 Jan;50(1):25-39. doi: 10.2165/11534740-000000000-00000. [PubMed:21142266 ]
  3. Scholler-Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM: Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. doi: 10.2165/10895940-000000000-00000. [PubMed:19725591 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Perez VE, Sanchez-Parra C, Serrano Villar S: [Etravirine drug interactions]. Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:27-31. doi: 10.1016/S0213-005X(09)73216-1. [PubMed:20116625 ]
  2. Kakuda TN, Scholler-Gyure M, Hoetelmans RM: Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet. 2011 Jan;50(1):25-39. doi: 10.2165/11534740-000000000-00000. [PubMed:21142266 ]
  3. Scholler-Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM: Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. doi: 10.2165/10895940-000000000-00000. [PubMed:19725591 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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
Molecular Weight:
141477.255 Da
References
  1. Kakuda TN, Scholler-Gyure M, Hoetelmans RM: Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet. 2011 Jan;50(1):25-39. doi: 10.2165/11534740-000000000-00000. [PubMed:21142266 ]
  2. Scholler-Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM: Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. doi: 10.2165/10895940-000000000-00000. [PubMed:19725591 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent phospholipid efflux translocator that acts as a positive regulator of biliary lipid secretion. Functions as a floppase that translocates specifically phosphatidylcholine (PC) from the inner to the outer leaflet of the canalicular membrane bilayer into the canaliculi of hepatocytes. Translocation of PC makes the biliary phospholipids available for extraction into the canaliculi ...
Gene Name:
ABCB4
Uniprot ID:
P21439
Molecular Weight:
141521.845 Da
References
  1. Kakuda TN, Scholler-Gyure M, Hoetelmans RM: Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet. 2011 Jan;50(1):25-39. doi: 10.2165/11534740-000000000-00000. [PubMed:21142266 ]
  2. Scholler-Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM: Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. doi: 10.2165/10895940-000000000-00000. [PubMed:19725591 ]
Comments
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Drug created on March 19, 2008 10:32 / Updated on May 28, 2016 02:12