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Identification
NameRilpivirine
Accession NumberDB08864
TypeSmall Molecule
GroupsApproved
Description

Rilpivirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) which is used for the treatment of HIV-1 infections in treatment-naive patients. It is a diarylpyrimidine, a class of molecules that resemble pyrimidine nucleotides found in DNA. Because of its flexible chemical structure, resistance of rilpivirine is less likely to develop than other NNRTI’s. FDA approved on May 20, 2011.

Structure
Thumb
Synonyms
4-{[4-({4-[(e)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
TMC 278
TMC278
External Identifiers
  • TMC278
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eduranttablet, film coated25 mg/1oralJanssen Products, LP2011-05-20Not applicableUs
Eduranttablet25 mgoralJanssen Inc2011-08-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
CompleraPhysicians Total Care, Inc.
OdefseyGilead Sciences, Inc.
Salts
Name/CASStructureProperties
Rilpivirine Hydrochloride
700361-47-3
Thumb
  • InChI Key: KZVVGZKAVZUACK-BJILWQEISA-N
  • Monoisotopic Mass: 402.135972345
  • Average Mass: 402.879
DBSALT000152
Categories
UNIINot Available
CAS number500287-72-9
WeightAverage: 366.4185
Monoisotopic: 366.159294606
Chemical FormulaC22H18N6
InChI KeyInChIKey=YIBOMRUWOWDFLG-ONEGZZNKSA-N
InChI
InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9,11-13H,1-2H3,(H2,25,26,27,28)/b4-3+
IUPAC Name
4-{[4-({4-[(1E)-2-cyanoeth-1-en-1-yl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
SMILES
CC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC2=CC=C(C=C2)C#N)=N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzonitriles. These are organic compounds containing a benzene bearing a nitrile substituent.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzonitriles
Direct ParentBenzonitriles
Alternative Parents
Substituents
  • Styrene
  • Benzonitrile
  • Aminopyrimidine
  • Imidolactam
  • Pyrimidine
  • Heteroaromatic compound
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Nitrile
  • Carbonitrile
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of HIV-1 infections in treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL in combination with at least 2 other antiretroviral agents.
PharmacodynamicsRilpivirine is the most potent NNRTI and has a EC50 of 0.73 nM in vitro against HIV-1 because its chemical structure allowed for better binding to reverse transcriptase.
Mechanism of actionRilpivirine is an NNRTI which binds to reverse transcriptase which results in a block in RNA and DNA- dependent DNA polymerase activities. One such activity is HIV-1 replication. Intracellular phosphorylation is not necessary for its antiviral activity. Because of the structure of rilpivirine is flexible around the aromatic rings, the molecule can have multiple conformations so that can bind to residues in the reverse transcriptase enzyme which have a lower mutation rate.
Related Articles
AbsorptionRilpivirine demonstrates dose-dependent pharmacokinetics and does not change between subscutaneous, IV, and intramuscular administration. Absorption increases with meals. Tmax, oral administration = 4 hours;
Volume of distributionNot Available
Protein binding>99% protein bound.
Metabolism

Mainly hepatically metabolized by CYP3A4. Because it is highly protein bound, its free plasma concentration is very small thus is unlikely to inhibit cytochrome proteins to a clinically relevant degree despite being an inhibitor of CYP3A4, CYP2C19, and CYP2B6.

Route of eliminationExcreted fecally (85%, 25% as unchanged drug) and urine (6%, <1% as unchanged drug)
Half life34-55 hours after oral administration
ClearanceNot Available
ToxicityOral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg.
Affected organisms
  • Human Immunodeficiency Virus
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9929
Blood Brain Barrier+0.8571
Caco-2 permeable+0.6609
P-glycoprotein substrateNon-substrate0.6933
P-glycoprotein inhibitor INon-inhibitor0.6604
P-glycoprotein inhibitor IINon-inhibitor0.7001
Renal organic cation transporterNon-inhibitor0.8261
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.8322
CYP450 3A4 substrateNon-substrate0.6778
CYP450 1A2 substrateInhibitor0.8256
CYP450 2C9 inhibitorNon-inhibitor0.9105
CYP450 2D6 inhibitorNon-inhibitor0.9202
CYP450 2C19 inhibitorNon-inhibitor0.806
CYP450 3A4 inhibitorNon-inhibitor0.9013
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5439
Ames testNon AMES toxic0.6229
CarcinogenicityNon-carcinogens0.9097
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8139 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9027
hERG inhibition (predictor II)Non-inhibitor0.841
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral
Tablet, film coatedoral
Tabletoral25 mg
Tablet, film coatedoral25 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5814639 Yes1996-03-292016-03-29Us
US5914331 Yes1998-01-022018-01-02Us
US5922695 Yes1998-01-252018-01-25Us
US5935946 Yes1998-01-252018-01-25Us
US5977089 Yes1998-01-252018-01-25Us
US6043230 Yes1998-01-252018-01-25Us
US6642245 Yes2001-05-042021-05-04Us
US6703396 Yes2001-09-092021-09-09Us
US6838464 No2001-02-262021-02-26Us
US7067522 No1999-12-202019-12-20Us
US7125879 No2002-08-092022-08-09Us
US7390791 No2002-05-072022-05-07Us
US7638522 No2003-04-142023-04-14Us
US7803788 No2002-02-022022-02-02Us
US8080551 No2003-04-112023-04-11Us
US8101629 No2002-08-092022-08-09Us
US8592397 No2004-01-132024-01-13Us
US8716264 No2004-01-132024-01-13Us
US8754065 No2012-08-152032-08-15Us
US8841310 No2005-12-092025-12-09Us
US9296769 No2012-08-152032-08-15Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point241-243°CSun, et al.: J. Med. Chem., 41, 4648 (1998), Kashiwada, et al.: Bioorg. Med. Chem. Lett., 11, 183 (2001)
Predicted Properties
PropertyValueSource
Water Solubility0.0116 mg/mLALOGPS
logP3.8ALOGPS
logP5.47ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)12.93ChemAxon
pKa (Strongest Basic)5.16ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area97.42 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity111.74 m3·mol-1ChemAxon
Polarizability40.65 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. Garvey L, Winston A: Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor. Expert Opin Investig Drugs. 2009 Jul;18(7):1035-41. doi: 10.1517/13543780903055056. [PubMed:19548857 ]
  2. Fernandez-Montero JV, Vispo E, Anta L, de Mendoza C, Soriano V: Rilpivirine: a next-generation non-nucleoside analogue for the treatment of HIV infection. Expert Opin Pharmacother. 2012 May;13(7):1007-14. doi: 10.1517/14656566.2012.667802. [PubMed:22519768 ]
  3. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
  4. Zaharatos GJ, Wainberg MA: Update on rilpivirine: a new potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV replication. Ann Med. 2013 May;45(3):236-41. doi: 10.3109/07853890.2012.732704. Epub 2012 Nov 17. [PubMed:23157601 ]
  5. Lexicomp 2013 [Link]
External Links
ATC CodesJ05AR19J05AG05J05AR08
AHFS Codes
  • 8:18.08.16
PDB EntriesNot Available
FDA labelDownload (558 KB)
MSDSDownload (568 KB)
Interactions
Drug Interactions
Drug
Aluminum hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum hydroxide.
AtazanavirThe serum concentration of Rilpivirine can be increased when it is combined with Atazanavir.
AzithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Azithromycin.
BexaroteneThe serum concentration of Rilpivirine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Rilpivirine can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Rilpivirine can be decreased when it is combined with Bosentan.
Calcium carbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Calcium carbonate.
CarbamazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Rilpivirine can be increased when it is combined with Ceritinib.
CimetidineThe serum concentration of Rilpivirine can be decreased when it is combined with Cimetidine.
CitalopramRilpivirine may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Rilpivirine can be increased when it is combined with Cobicistat.
DabrafenibThe serum concentration of Rilpivirine can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Rilpivirine can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Rilpivirine can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Rilpivirine can be increased when it is combined with Delavirdine.
DexamethasoneThe serum concentration of Rilpivirine can be decreased when it is combined with Dexamethasone.
DidanosineRilpivirine can cause a decrease in the absorption of Didanosine resulting in a reduced serum concentration and potentially a decrease in efficacy.
DofetilideRilpivirine may increase the QTc-prolonging activities of Dofetilide.
EfavirenzThe serum concentration of Rilpivirine can be increased when it is combined with Efavirenz.
ErythromycinThe serum concentration of Rilpivirine can be increased when it is combined with Erythromycin.
EsomeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Esomeprazole.
EtravirineThe serum concentration of Rilpivirine can be increased when it is combined with Etravirine.
FamotidineThe serum concentration of Rilpivirine can be decreased when it is combined with Famotidine.
FidaxomicinThe serum concentration of Rilpivirine can be increased when it is combined with Fidaxomicin.
FosphenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Fosphenytoin.
GoserelinRilpivirine may increase the QTc-prolonging activities of Goserelin.
IdelalisibThe serum concentration of Rilpivirine can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Rilpivirine can be increased when it is combined with Indinavir.
ItraconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Lansoprazole.
LeuprolideRilpivirine may increase the QTc-prolonging activities of Leuprolide.
LopinavirThe serum concentration of Rilpivirine can be increased when it is combined with Lopinavir.
Magnesium hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium oxide.
MethadoneThe metabolism of Methadone can be increased when combined with Rilpivirine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Rilpivirine.
MitotaneThe serum concentration of Rilpivirine can be decreased when it is combined with Mitotane.
NefazodoneThe serum concentration of Rilpivirine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Rilpivirine can be increased when it is combined with Nelfinavir.
NevirapineThe serum concentration of Rilpivirine can be increased when it is combined with Nevirapine.
NizatidineThe serum concentration of Rilpivirine can be decreased when it is combined with Nizatidine.
OmeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Omeprazole.
OxcarbazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Oxcarbazepine.
PantoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Pantoprazole.
PhenobarbitalThe serum concentration of Rilpivirine can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Phenytoin.
PosaconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Rilpivirine can be decreased when it is combined with Primidone.
RabeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Rabeprazole.
RanitidineThe serum concentration of Rilpivirine can be decreased when it is combined with Ranitidine.
RifabutinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Rilpivirine can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Rilpivirine can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Rilpivirine can be increased when it is combined with Saquinavir.
SiltuximabThe serum concentration of Rilpivirine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Rilpivirine can be increased when it is combined with Simeprevir.
Sodium bicarbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Sodium bicarbonate.
SpiramycinThe serum concentration of Rilpivirine can be increased when it is combined with Spiramycin.
St. John's WortThe serum concentration of Rilpivirine can be decreased when it is combined with St. John&#39;s Wort.
TelaprevirThe serum concentration of Rilpivirine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Telithromycin.
TocilizumabThe serum concentration of Rilpivirine can be decreased when it is combined with Tocilizumab.
VoriconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Voriconazole.
Food Interactions
  • Absorption is increased by 40% if taken with food.
  • Co-administration with St. John's wort decreases levels of rilpivirine by inducing CYP3A4 metabolism. Use is contraindicated.

Targets

Kind
Protein
Organism
Human immunodeficiency virus 1
Pharmacological action
yes
Actions
inhibitor
General Function:
Rna-dna hybrid ribonuclease activity
Specific Function:
Not Available
Gene Name:
pol
Uniprot ID:
Q72547
Molecular Weight:
65223.615 Da
References
  1. Garvey L, Winston A: Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor. Expert Opin Investig Drugs. 2009 Jul;18(7):1035-41. doi: 10.1517/13543780903055056. [PubMed:19548857 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and is...
Gene Name:
NR1I2
Uniprot ID:
O75469
Molecular Weight:
49761.245 Da
References
  1. Sharma D, Lau AJ, Sherman MA, Chang TK: Agonism of human pregnane X receptor by rilpivirine and etravirine: comparison with first generation non-nucleoside reverse transcriptase inhibitors. Biochem Pharmacol. 2013 Jun 1;85(11):1700-11. doi: 10.1016/j.bcp.2013.04.002. Epub 2013 Apr 9. [PubMed:23583259 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrateinhibitorinducer
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. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]

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. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Weiss J, Haefeli WE: Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. doi: 10.1016/j.ijantimicag.2013.01.004. Epub 2013 Feb 18. [PubMed:23428312 ]
Comments
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Drug created on March 14, 2013 15:23 / Updated on August 24, 2016 03:05