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Identification
NameRilpivirine
Accession NumberDB08864  (DB08592, DB05083)
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
External Identifiers
  • TMC 278
  • TMC278
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EdurantTablet25 mgOralJanssen Inc2011-08-31Not applicableCanada
EdurantTablet, film coated25 mgOralJanssen Cilag International N.V.2011-11-28Not applicableEu
EdurantTablet, film coated25 mg/1OralJanssen Products, LP2011-05-20Not applicableUs
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
UNIIFI96A8X663
CAS number500287-72-9
WeightAverage: 366.4185
Monoisotopic: 366.159294606
Chemical FormulaC22H18N6
InChI KeyYIBOMRUWOWDFLG-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
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.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Reverse transcriptase/RNaseHProteinyes
inhibitor
Human immunodeficiency virus 1Q72547 details
Nuclear receptor subfamily 1 group I member 2Proteinunknown
agonist
HumanO75469 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Rilpivirine.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Rilpivirine.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Rilpivirine.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Rilpivirine.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Rilpivirine.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Rilpivirine.Approved, Investigational
Aluminum hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum hydroxide.Approved
Aluminum phosphateThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum phosphate.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Rilpivirine.Approved, Investigational
AmiodaroneThe serum concentration of Rilpivirine can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Rilpivirine.Approved
AnagrelideRilpivirine may increase the QTc-prolonging activities of Anagrelide.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Rilpivirine.Approved
AprepitantThe serum concentration of Rilpivirine can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Rilpivirine.Approved, Investigational
Arsenic trioxideRilpivirine may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherRilpivirine may increase the QTc-prolonging activities of Artemether.Approved
AsenapineThe serum concentration of Rilpivirine can be decreased when it is combined with Asenapine.Approved
AtazanavirThe serum concentration of Rilpivirine can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Rilpivirine.Approved
AtomoxetineThe metabolism of Rilpivirine can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Rilpivirine.Approved, Investigational
AzithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Azithromycin.Approved
BedaquilineRilpivirine may increase the QTc-prolonging activities of Bedaquiline.Approved
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
BexaroteneThe serum concentration of Rilpivirine can be decreased when it is combined with Bexarotene.Approved, Investigational
Bismuth SubcitrateThe serum concentration of Rilpivirine can be decreased when it is combined with Bismuth Subcitrate.Approved
BoceprevirThe serum concentration of Rilpivirine can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Rilpivirine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Rilpivirine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Rilpivirine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Rilpivirine.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Rilpivirine.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Rilpivirine.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Rilpivirine.Approved
Calcium carbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Calcium carbonate.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Rilpivirine.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Rilpivirine.Approved
CarbamazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Rilpivirine can be increased when it is combined with Carbomycin.Vet Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Rilpivirine.Approved
CeritinibThe serum concentration of Rilpivirine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Rilpivirine.Withdrawn
ChloroquineRilpivirine may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineRilpivirine may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Rilpivirine.Approved
CimetidineThe serum concentration of Rilpivirine can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinRilpivirine may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideRilpivirine may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Rilpivirine.Approved
CitalopramRilpivirine may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Rilpivirine can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Rilpivirine.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Rilpivirine.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Rilpivirine.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Rilpivirine.Approved, Nutraceutical
ClotrimazoleThe metabolism of Rilpivirine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineRilpivirine may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe serum concentration of Rilpivirine can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Rilpivirine.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Rilpivirine.Approved
ConivaptanThe serum concentration of Rilpivirine can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Rilpivirine.Approved
CrizotinibRilpivirine may increase the QTc-prolonging activities of Crizotinib.Approved
CyclosporineThe metabolism of Rilpivirine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Rilpivirine.Approved
DabrafenibThe serum concentration of Rilpivirine can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Rilpivirine.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Rilpivirine.Approved
DarunavirThe serum concentration of Rilpivirine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Rilpivirine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Rilpivirine.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Rilpivirine.Approved
DeferasiroxThe serum concentration of Rilpivirine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Rilpivirine can be increased when it is combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Rilpivirine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Rilpivirine.Approved, Illicit, Vet Approved
DidanosineRilpivirine can cause a decrease in the absorption of Didanosine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Rilpivirine.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Rilpivirine.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Rilpivirine.Approved
DihydroergotamineThe metabolism of Rilpivirine can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Rilpivirine.Illicit
DiltiazemThe metabolism of Rilpivirine can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Rilpivirine.Approved
DisopyramideRilpivirine may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Rilpivirine.Approved, Investigational
DofetilideRilpivirine may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronRilpivirine may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneRilpivirine may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxepinThe serum concentration of Rilpivirine can be decreased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Rilpivirine.Approved, Investigational
DoxycyclineThe metabolism of Rilpivirine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneRilpivirine may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolRilpivirine may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Rilpivirine.Approved
EfavirenzThe serum concentration of Rilpivirine can be increased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Rilpivirine.Approved, Investigational
EliglustatRilpivirine may increase the QTc-prolonging activities of Eliglustat.Approved
EnzalutamideThe serum concentration of Rilpivirine can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Rilpivirine can be decreased when it is combined with Epinastine.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Rilpivirine.Approved, Investigational
ErythromycinThe serum concentration of Rilpivirine can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramRilpivirine may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Esomeprazole.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Rilpivirine.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Rilpivirine.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Rilpivirine.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Rilpivirine.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Rilpivirine.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Rilpivirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Rilpivirine.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Rilpivirine.Approved
FamotidineThe serum concentration of Rilpivirine can be decreased when it is combined with Famotidine.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Rilpivirine.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Rilpivirine.Approved
FidaxomicinThe serum concentration of Rilpivirine can be increased when it is combined with Fidaxomicin.Approved
FlecainideRilpivirine may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleThe metabolism of Rilpivirine can be decreased when combined with Fluconazole.Approved
FluoxetineRilpivirine may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolRilpivirine may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Rilpivirine.Approved
FluvoxamineThe metabolism of Rilpivirine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Rilpivirine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rilpivirine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Rilpivirine can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidRilpivirine may increase the QTc-prolonging activities of Gadobenic acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Rilpivirine.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Rilpivirine.Approved
GemifloxacinRilpivirine may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GoserelinRilpivirine may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronRilpivirine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Rilpivirine.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Rilpivirine.Withdrawn
HaloperidolRilpivirine may increase the QTc-prolonging activities of Haloperidol.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Rilpivirine.Approved
IbutilideRilpivirine may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Rilpivirine can be increased when it is combined with Idelalisib.Approved
IloperidoneRilpivirine may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Rilpivirine can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Rilpivirine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Rilpivirine.Approved
IndinavirThe serum concentration of Rilpivirine can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Rilpivirine.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Rilpivirine.Approved, Investigational
IsavuconazoniumThe metabolism of Rilpivirine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Rilpivirine can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Rilpivirine can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Rilpivirine.Approved, Vet Approved
JosamycinThe serum concentration of Rilpivirine can be increased when it is combined with Josamycin.Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Rilpivirine.Approved
KetoconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Rilpivirine can be increased when it is combined with Kitasamycin.Experimental
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Rilpivirine.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Rilpivirine.Approved, Investigational
LansoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Lansoprazole.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Rilpivirine.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Rilpivirine.Approved
LenvatinibRilpivirine may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideRilpivirine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Rilpivirine.Approved, Investigational
LevofloxacinRilpivirine may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Rilpivirine.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Rilpivirine.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Rilpivirine.Approved
LopinavirThe serum concentration of Rilpivirine can be increased when it is combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Rilpivirine.Approved
LovastatinThe metabolism of Rilpivirine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Rilpivirine can be increased when combined with Lumacaftor.Approved
LumefantrineRilpivirine may increase the QTc-prolonging activities of Lumefantrine.Approved
MagaldrateThe serum concentration of Rilpivirine can be decreased when it is combined with Magaldrate.Withdrawn
Magnesium carbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium carbonate.Approved
Magnesium hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium hydroxide.Approved
Magnesium oxideThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium oxide.Approved
Magnesium TrisilicateThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium Trisilicate.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Rilpivirine.Approved, Investigational
MethadoneThe metabolism of Methadone can be increased when combined with Rilpivirine.Approved
MethanthelineThe serum concentration of Rilpivirine can be decreased when it is combined with Methantheline.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Rilpivirine.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
MetiamideThe serum concentration of Rilpivirine can be decreased when it is combined with Metiamide.Experimental
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Rilpivirine.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Rilpivirine.Approved, Illicit
MifepristoneMifepristone may increase the QTc-prolonging activities of Rilpivirine.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Rilpivirine.Approved
MitotaneThe serum concentration of Rilpivirine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Rilpivirine.Approved, Investigational
ModafinilThe serum concentration of Rilpivirine can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Rilpivirine.Approved, Investigational
MoxifloxacinRilpivirine may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Rilpivirine.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Rilpivirine.Approved
NafcillinThe serum concentration of Rilpivirine can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Rilpivirine.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
NefazodoneThe serum concentration of Rilpivirine can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Rilpivirine can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Rilpivirine can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Rilpivirine can be increased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Rilpivirine.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Rilpivirine.Approved
NilotinibRilpivirine may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Rilpivirine.Approved
NizatidineThe serum concentration of Rilpivirine can be decreased when it is combined with Nizatidine.Approved
OfloxacinRilpivirine may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Rilpivirine can be decreased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Rilpivirine can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Rilpivirine can be increased when it is combined with Oleandomycin.Vet Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Rilpivirine.Approved
OmeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronRilpivirine may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Rilpivirine can be increased when it is combined with Osimertinib.Approved
OxcarbazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Oxcarbazepine.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Rilpivirine.Approved, Vet Approved
PalbociclibThe serum concentration of Rilpivirine can be increased when it is combined with Palbociclib.Approved
PaliperidoneRilpivirine may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatRilpivirine may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Pantoprazole.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Rilpivirine.Approved
PentamidineRilpivirine may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalThe metabolism of Rilpivirine can be increased when combined with Pentobarbital.Approved, Vet Approved
PerflutrenRilpivirine may increase the QTc-prolonging activities of Perflutren.Approved
PhenobarbitalThe serum concentration of Rilpivirine can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideRilpivirine may increase the QTc-prolonging activities of Pimozide.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rilpivirine.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Rilpivirine.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Rilpivirine.Approved
PosaconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Rilpivirine.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Rilpivirine.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
PrimaquineRilpivirine may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe serum concentration of Rilpivirine can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideRilpivirine may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Rilpivirine.Approved, Vet Approved
PromazineRilpivirine may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneRilpivirine may increase the QTc-prolonging activities of Propafenone.Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Rilpivirine.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Rilpivirine.Approved
QuetiapineRilpivirine may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineRilpivirine may increase the QTc-prolonging activities of Quinidine.Approved
QuinineRilpivirine may increase the QTc-prolonging activities of Quinine.Approved
RabeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Rabeprazole.Approved, Investigational
RanitidineThe serum concentration of Rilpivirine can be decreased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Rilpivirine.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Rilpivirine.Approved
RifabutinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Rilpivirine can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Rilpivirine.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Rilpivirine.Approved, Investigational
RitonavirThe serum concentration of Rilpivirine can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Rilpivirine.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Rilpivirine.Approved, Investigational
Roxatidine acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Roxatidine acetate.Approved
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Rilpivirine.Approved, Vet Approved
SaquinavirThe serum concentration of Rilpivirine can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rilpivirine.Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Rilpivirine.Approved
SildenafilThe metabolism of Rilpivirine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Rilpivirine.Approved
SiltuximabThe serum concentration of Rilpivirine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Rilpivirine can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Rilpivirine.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Rilpivirine.Approved
SolithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Solithromycin.Investigational
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Rilpivirine.Approved, Investigational
SotalolRilpivirine may increase the QTc-prolonging activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Rilpivirine.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Rilpivirine.Experimental
SpiramycinThe serum concentration of Rilpivirine can be increased when it is combined with Spiramycin.Approved
St. John's WortThe serum concentration of Rilpivirine can be decreased when it is combined with St. John&#39;s Wort.Nutraceutical
StiripentolThe serum concentration of Rilpivirine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleRilpivirine may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine.Approved, Investigational
TAK-390MRThe serum concentration of Rilpivirine can be decreased when it is combined with TAK-390MR.Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Rilpivirine.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Rilpivirine.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Rilpivirine.Approved
TelaprevirThe serum concentration of Rilpivirine can be increased when it is combined with Telaprevir.Approved
TelavancinRilpivirine may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Rilpivirine.Approved
TetrabenazineRilpivirine may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineRilpivirine may increase the QTc-prolonging activities of Thioridazine.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Rilpivirine.Approved
TiclopidineThe metabolism of Rilpivirine can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Rilpivirine.Approved
TocilizumabThe serum concentration of Rilpivirine can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Rilpivirine.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Rilpivirine.Approved, Investigational
ToremifeneRilpivirine may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Rilpivirine.Approved
TroleandomycinThe serum concentration of Rilpivirine can be increased when it is combined with Troleandomycin.Approved
TylosinThe serum concentration of Rilpivirine can be increased when it is combined with Tylosin.Vet Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Rilpivirine.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Rilpivirine.Approved
VandetanibRilpivirine may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Rilpivirine.Approved
VemurafenibRilpivirine may increase the QTc-prolonging activities of Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Rilpivirine.Approved
VenlafaxineThe metabolism of Rilpivirine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Rilpivirine can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Rilpivirine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Rilpivirine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Rilpivirine.Approved
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Rilpivirine.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Rilpivirine.Approved
ZiprasidoneRilpivirine may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolRilpivirine may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
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.
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 CodesNot Available
AHFS Codes
  • 8:18.08.16
PDB Entries
FDA labelDownload (558 KB)
MSDSDownload (568 KB)
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
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
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

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 December 07, 2016 03:54