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Identification
NameRilpivirine
Accession NumberDB08864
TypeSmall Molecule
GroupsApproved
DescriptionRilpivirine 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
EdurantFilm-coated tablet Page 1 of 125 mgOral useJanssen Cilag International N.V.2011-11-28Not applicableEu
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
Film-coated tablet page 1 of 1Oral use25 mg
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
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Rilpivirine.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Rilpivirine.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Rilpivirine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Rilpivirine.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Rilpivirine.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Rilpivirine.
Aluminum hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum phosphate.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Rilpivirine.
AmiodaroneThe serum concentration of Rilpivirine can be increased when it is combined with Amiodarone.
AmiodaroneRilpivirine may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Rilpivirine.
AnagrelideRilpivirine may increase the QTc-prolonging activities of Anagrelide.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Rilpivirine.
AprepitantThe serum concentration of Rilpivirine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rilpivirine.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Rilpivirine.
ArtemetherRilpivirine may increase the QTc-prolonging activities of Artemether.
AsenapineThe serum concentration of Rilpivirine can be decreased when it is combined with Asenapine.
AsenapineRilpivirine may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe serum concentration of Rilpivirine can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Rilpivirine.
AtomoxetineThe metabolism of Rilpivirine can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Rilpivirine.
AzithromycinRilpivirine may increase the QTc-prolonging activities of Azithromycin.
BedaquilineRilpivirine may increase the QTc-prolonging activities of Bedaquiline.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Rilpivirine.
BexaroteneThe serum concentration of Rilpivirine can be decreased when it is combined with Bexarotene.
Bismuth SubcitrateThe serum concentration of Rilpivirine can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Rilpivirine can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Rilpivirine can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Rilpivirine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Rilpivirine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Rilpivirine.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Rilpivirine.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Rilpivirine.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Rilpivirine.
Calcium carbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Calcium carbonate.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Rilpivirine.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Rilpivirine.
CarbamazepineThe metabolism of Rilpivirine can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Rilpivirine.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Rilpivirine.
CeritinibThe serum concentration of Rilpivirine can be increased when it is combined with Ceritinib.
CeritinibRilpivirine may increase the QTc-prolonging activities of Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Rilpivirine.
ChloroquineRilpivirine may increase the QTc-prolonging activities of Chloroquine.
ChlorpromazineRilpivirine may increase the QTc-prolonging activities of Chlorpromazine.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Rilpivirine.
CimetidineThe serum concentration of Rilpivirine can be decreased when it is combined with Cimetidine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Rilpivirine.
CiprofloxacinRilpivirine may increase the QTc-prolonging activities of Ciprofloxacin.
CisaprideRilpivirine may increase the QTc-prolonging activities of Cisapride.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Rilpivirine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Rilpivirine.
ClarithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Clarithromycin.
ClarithromycinRilpivirine may increase the QTc-prolonging activities of Clarithromycin.
ClemastineThe metabolism of Rilpivirine can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Rilpivirine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Rilpivirine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Rilpivirine.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Rilpivirine.
ClotrimazoleThe metabolism of Rilpivirine can be decreased when combined with Clotrimazole.
ClozapineRilpivirine may increase the QTc-prolonging activities of Clozapine.
CobicistatThe serum concentration of Rilpivirine can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Rilpivirine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Rilpivirine.
ConivaptanThe serum concentration of Rilpivirine can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Rilpivirine.
CrizotinibRilpivirine may increase the QTc-prolonging activities of Crizotinib.
CrizotinibThe metabolism of Rilpivirine can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Rilpivirine can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Rilpivirine.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Rilpivirine.
DabrafenibThe serum concentration of Rilpivirine can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Rilpivirine.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Rilpivirine.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Rilpivirine.
DarunavirThe serum concentration of Rilpivirine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Rilpivirine can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Rilpivirine.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Rilpivirine.
DeferasiroxThe serum concentration of Rilpivirine can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Rilpivirine can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Rilpivirine can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Rilpivirine.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Rilpivirine.
DidanosineRilpivirine can cause a decrease in the absorption of Didanosine resulting in a reduced serum concentration and potentially a decrease in efficacy.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Rilpivirine.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Rilpivirine.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Rilpivirine.
DihydroergotamineThe metabolism of Rilpivirine can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Rilpivirine.
DiltiazemThe metabolism of Rilpivirine can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Rilpivirine.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Rilpivirine.
DisopyramideRilpivirine may increase the QTc-prolonging activities of Disopyramide.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Rilpivirine.
DofetilideRilpivirine may increase the QTc-prolonging activities of Dofetilide.
DolasetronRilpivirine may increase the QTc-prolonging activities of Dolasetron.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Rilpivirine.
DoxepinThe serum concentration of Rilpivirine can be decreased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Rilpivirine.
DoxycyclineThe metabolism of Rilpivirine can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Rilpivirine can be decreased when combined with Dronedarone.
DronedaroneRilpivirine may increase the QTc-prolonging activities of Dronedarone.
DroperidolRilpivirine may increase the QTc-prolonging activities of Droperidol.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Rilpivirine.
EfavirenzThe serum concentration of Rilpivirine can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Rilpivirine.
EliglustatRilpivirine may increase the QTc-prolonging activities of Eliglustat.
EnzalutamideThe serum concentration of Rilpivirine can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Rilpivirine can be decreased when it is combined with Epinastine.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Rilpivirine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Rilpivirine.
ErythromycinRilpivirine may increase the QTc-prolonging activities of Erythromycin.
ErythromycinThe metabolism of Rilpivirine can be decreased when combined with Erythromycin.
EscitalopramRilpivirine may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Esomeprazole.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Rilpivirine.
EstriolThe serum concentration of Estriol can be increased when it is combined with Rilpivirine.
EstroneThe serum concentration of Estrone can be increased when it is combined with Rilpivirine.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Rilpivirine.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Rilpivirine.
EtravirineThe serum concentration of Rilpivirine can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Rilpivirine.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Rilpivirine.
FamotidineThe serum concentration of Rilpivirine can be decreased when it is combined with Famotidine.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Rilpivirine.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Rilpivirine.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Rilpivirine.
FlecainideRilpivirine may increase the QTc-prolonging activities of Flecainide.
FluconazoleThe metabolism of Rilpivirine can be decreased when combined with Fluconazole.
FluoxetineRilpivirine may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolRilpivirine may increase the QTc-prolonging activities of Flupentixol.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Rilpivirine.
FluvoxamineThe metabolism of Rilpivirine can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Rilpivirine can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Rilpivirine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Rilpivirine can be increased when it is combined with Fusidic Acid.
Gadobenic acidRilpivirine may increase the QTc-prolonging activities of Gadobenic acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Rilpivirine.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Rilpivirine.
GemifloxacinRilpivirine may increase the QTc-prolonging activities of Gemifloxacin.
GoserelinRilpivirine may increase the QTc-prolonging activities of Goserelin.
GranisetronRilpivirine may increase the QTc-prolonging activities of Granisetron.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Rilpivirine.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Rilpivirine.
HaloperidolRilpivirine may increase the QTc-prolonging activities of Haloperidol.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Rilpivirine.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Rilpivirine.
IbutilideRilpivirine may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Rilpivirine can be increased when it is combined with Idelalisib.
IloperidoneRilpivirine may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Rilpivirine can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Rilpivirine.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Rilpivirine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Rilpivirine.
IndinavirThe serum concentration of Rilpivirine can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Rilpivirine.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Rilpivirine.
IsavuconazoniumThe metabolism of Rilpivirine can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Rilpivirine can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Rilpivirine can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Rilpivirine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Rilpivirine.
KetoconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Rilpivirine.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Rilpivirine.
LansoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Lansoprazole.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Rilpivirine.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Rilpivirine.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Rilpivirine.
LenvatinibRilpivirine may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideRilpivirine may increase the QTc-prolonging activities of Leuprolide.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Rilpivirine.
LevofloxacinRilpivirine may increase the QTc-prolonging activities of Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Rilpivirine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Rilpivirine.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Rilpivirine.
LopinavirThe serum concentration of Rilpivirine can be increased when it is combined with Lopinavir.
LopinavirRilpivirine may increase the QTc-prolonging activities of Lopinavir.
LosartanThe serum concentration of Losartan can be increased when it is combined with Rilpivirine.
LovastatinThe metabolism of Rilpivirine can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Luliconazole.
LumefantrineRilpivirine may increase the QTc-prolonging activities of Lumefantrine.
MagaldrateThe serum concentration of Rilpivirine can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium carbonate.
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.
Magnesium TrisilicateThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium Trisilicate.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Rilpivirine.
MethadoneRilpivirine may increase the QTc-prolonging activities of Methadone.
MethanthelineThe serum concentration of Rilpivirine can be decreased when it is combined with Methantheline.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Rilpivirine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Rilpivirine.
MetiamideThe serum concentration of Rilpivirine can be decreased when it is combined with Metiamide.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Rilpivirine.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Rilpivirine.
MifepristoneThe metabolism of Rilpivirine can be decreased when combined with Mifepristone.
MifepristoneRilpivirine may increase the QTc-prolonging activities of Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Rilpivirine.
MitotaneThe serum concentration of Rilpivirine can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Rilpivirine.
ModafinilThe serum concentration of Rilpivirine can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Rilpivirine.
MoxifloxacinRilpivirine may increase the QTc-prolonging activities of Moxifloxacin.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Rilpivirine.
NadololThe serum concentration of Nadolol can be increased when it is combined with Rilpivirine.
NafcillinThe serum concentration of Rilpivirine can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Rilpivirine.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Rilpivirine.
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.
NetupitantThe serum concentration of Rilpivirine can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Rilpivirine can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Rilpivirine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Rilpivirine.
NilotinibThe metabolism of Rilpivirine can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Rilpivirine.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Rilpivirine.
NizatidineThe serum concentration of Rilpivirine can be decreased when it is combined with Nizatidine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Rilpivirine.
OfloxacinRilpivirine may increase the QTc-prolonging activities of Ofloxacin.
OlanzapineThe serum concentration of Rilpivirine can be decreased when it is combined with Olanzapine.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Rilpivirine.
OlaparibThe metabolism of Rilpivirine can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Rilpivirine.
OmeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Omeprazole.
OndansetronRilpivirine may increase the QTc-prolonging activities of Ondansetron.
OsimertinibThe serum concentration of Rilpivirine can be increased when it is combined with Osimertinib.
OxcarbazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Oxcarbazepine.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Rilpivirine.
PalbociclibThe serum concentration of Rilpivirine can be increased when it is combined with Palbociclib.
PaliperidoneRilpivirine may increase the QTc-prolonging activities of Paliperidone.
PanobinostatRilpivirine may increase the QTc-prolonging activities of Panobinostat.
PantoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Pantoprazole.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Rilpivirine.
PentamidineRilpivirine may increase the QTc-prolonging activities of Pentamidine.
PentobarbitalThe metabolism of Rilpivirine can be increased when combined with Pentobarbital.
PerflutrenRilpivirine may increase the QTc-prolonging activities of Perflutren.
PhenobarbitalThe serum concentration of Rilpivirine can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Rilpivirine.
PhenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Rilpivirine.
PimozideRilpivirine may increase the QTc-prolonging activities of Pimozide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rilpivirine.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Rilpivirine.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Rilpivirine.
PosaconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Rilpivirine.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Rilpivirine.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Rilpivirine.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Rilpivirine.
PrimaquineRilpivirine may increase the QTc-prolonging activities of Primaquine.
PrimidoneThe serum concentration of Rilpivirine can be decreased when it is combined with Primidone.
ProcainamideRilpivirine may increase the QTc-prolonging activities of Procainamide.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Rilpivirine.
PromazineRilpivirine may increase the QTc-prolonging activities of Promazine.
PropafenoneRilpivirine may increase the QTc-prolonging activities of Propafenone.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Rilpivirine.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Rilpivirine.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Rilpivirine.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Rilpivirine.
QuinineThe serum concentration of Quinine can be increased when it is combined with Rilpivirine.
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.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Rilpivirine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Rilpivirine.
RanolazineThe metabolism of Rilpivirine can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Rilpivirine.
RifabutinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifabutin.
RifampicinThe metabolism of Rilpivirine can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Rilpivirine.
RifapentineThe metabolism of Rilpivirine can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Rilpivirine can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Rilpivirine.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Rilpivirine.
Roxatidine acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Roxatidine acetate.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Rilpivirine.
SaquinavirThe serum concentration of Rilpivirine can be increased when it is combined with Saquinavir.
SaquinavirRilpivirine may increase the QTc-prolonging activities of Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rilpivirine.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Rilpivirine.
SildenafilThe metabolism of Rilpivirine can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Rilpivirine.
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.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Rilpivirine.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Rilpivirine.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Rilpivirine.
SotalolRilpivirine may increase the QTc-prolonging activities of Sotalol.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Rilpivirine.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Rilpivirine.
St. John's WortThe serum concentration of Rilpivirine can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Rilpivirine can be increased when it is combined with Stiripentol.
SulfisoxazoleRilpivirine may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Rilpivirine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine.
TAK-390MRThe serum concentration of Rilpivirine can be decreased when it is combined with TAK-390MR.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Rilpivirine.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Rilpivirine.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Rilpivirine.
TelaprevirThe serum concentration of Rilpivirine can be increased when it is combined with Telaprevir.
TelavancinRilpivirine may increase the QTc-prolonging activities of Telavancin.
TelithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Telithromycin.
TelithromycinRilpivirine may increase the QTc-prolonging activities of Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Rilpivirine.
TetrabenazineRilpivirine may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineRilpivirine may increase the QTc-prolonging activities of Thioridazine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Rilpivirine.
TiclopidineThe metabolism of Rilpivirine can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Rilpivirine.
TocilizumabThe serum concentration of Rilpivirine can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Rilpivirine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Rilpivirine.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Rilpivirine.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rilpivirine.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Rilpivirine.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Rilpivirine.
VandetanibRilpivirine may increase the QTc-prolonging activities of Vandetanib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Rilpivirine.
VemurafenibRilpivirine may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Rilpivirine can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Rilpivirine.
VerapamilThe metabolism of Rilpivirine can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Rilpivirine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Rilpivirine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Rilpivirine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Rilpivirine.
VoriconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Voriconazole.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Rilpivirine.
ZiprasidoneThe metabolism of Rilpivirine can be decreased when combined with Ziprasidone.
ZiprasidoneRilpivirine may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolRilpivirine may increase the QTc-prolonging activities of Zuclopenthixol.
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 ]
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Drug created on March 14, 2013 15:23 / Updated on September 30, 2016 03:38