Identification

Name
Rilpivirine
Accession Number
DB08864  (DB08592, DB05083)
Type
Small Molecule
Groups
Approved
Description

Rilpivirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) which is used for the treatment of HIV-1 infections in treatment-naive patients.[5] It is a diarylpyrimidine derivative, a class of molecules that resemble pyrimidine nucleotides found in DNA.[6] The internal conformational flexibility of rilpivirine and the plasticity of it interacting binding site gives it a very high potency and an unlikely generation of resistance compared to other NNRTI's.[7] Rilpivirine was developed by Tilbotec, Inc. and FDA approved on May 20, 2011.[10] On November 21, 2017, Rilpivirine, in combination with dolutegravir, was approved as part of the first complete treatment regimen with only two drugs for the treatment of adults with HIV-1 named Juluca.[11]

Structure
Thumb
Synonyms
  • 4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
External IDs
R 278474 / R-278474 / TMC 278 / TMC-278 / TMC278
Product Ingredients
IngredientUNIICASInChI Key
Rilpivirine Hydrochloride212WAX8KDD700361-47-3KZVVGZKAVZUACK-BJILWQEISA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EdurantTablet25 mgOralJanssen Pharmaceuticals2011-08-31Not applicableCanada
EdurantTablet, film coated25 mg/1OralJanssen, Lp2011-05-20Not applicableUs
EdurantTablet, film coated25 mgOralJanssen Cilag International Nv2011-11-28Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
CompleraRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2013-02-01Not applicableUs
CompleraRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralGilead Sciences2011-08-10Not applicableUs
CompleraRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralA S Medication Solutions2011-08-10Not applicableUs
CompleraRilpivirine (25 mg) + Emtricitabine (200 mg) + Tenofovir disoproxil fumarate (300 mg)TabletOralGilead Sciences2011-10-20Not applicableCanada
CompleraRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralRemedy Repack2017-08-16Not applicableUs
CompleraRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralA S Medication Solutions2011-08-102017-06-20Us
JulucaRilpivirine Hydrochloride (25 mg/1) + Dolutegravir Sodium (50 mg/1)Tablet, film coatedOralViiV Healthcare ULC2017-11-21Not applicableUs
OdefseyRilpivirine Hydrochloride (25 mg) + Emtricitabine (200 mg) + Tenofovir alafenamide (25 mg)Tablet, film coatedOralGilead Sciences Ireland Uc2016-06-21Not applicableEu
OdefseyRilpivirine Hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir alafenamide fumarate (25 mg/1)TabletOralRemedy Repack2017-08-17Not applicableUs
OdefseyRilpivirine Hydrochloride (25 mg) + Emtricitabine (200 mg) + Tenofovir alafenamide (25 mg)Tablet, film coatedOralGilead Sciences Ireland Uc2016-06-21Not applicableEu
Categories
UNII
FI96A8X663
CAS number
500287-72-9
Weight
Average: 366.4185
Monoisotopic: 366.159294606
Chemical Formula
C22H18N6
InChI Key
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

Pharmacology

Indication

Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm3.[10] The FDA combination therapy approval of rilpivirine and dolutegravir is indicated for adults with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy.[11]

Associated Conditions
Pharmacodynamics

Ripivirine treatment produces a significant and effective reduction in the viral load based on the study of HIV-1 RNA copies per ml or immunologic changes by the determination of counts of CD4+ and CD8+ cells.[12] The combinantion therapy (ripivirine and dolutegravir) presented the same viral supression found in previous three-drug therapies without integrase strand transfer inhibitor mutations or rilpivirine resistance.[13]

Mechanism of action

Rilpivirine is a non-competitive NNRTI that binds to reverse transcriptase. Its binding results in the blockage of RNA and DNA- dependent DNA polymerase activities, like HIV-1 replication. It does not present activity against human DNA polymerases α, β and γ.[12] Rilpivirine binds to the HIV-1 reverse transcriptase (RT) and its flexible structure around the aromatic rings allows the adaptation to changes in the non-nucleoside RT binding pocket.[8]

TargetActionsOrganism
AReverse transcriptase/RNaseH
inhibitor
Human immunodeficiency virus 1
UNuclear receptor subfamily 1 group I member 2
agonist
Human
Absorption

Absorption of rilpivirine is characterized by a lag time followed by a linear increase in plasma concentration. Under fasting conditions, the Cmax of rilpivirine can be decreased even by 46% while its AUC can be reduced by 43%. When given with a protein-rich drink the Cmax and AUC of rilpivirine is decreased by 50%. Therefore, it is recommended to consume rilpiviridine with a non-protein-rich meal. The average Tmax of various rilpivirine concentrations is 3-4 h.[7] The reported AUC in patients from clinical studies is 2235 ng h/ml.[Label]

Volume of distribution

In VIH-1 patients, the apparent volume of distribution in the central compartment was determined to be 152-173 L.[12]

Protein binding

Rilpivirine is highly protein-bound thus, >99% of its dose can be bound to plasma protein in a concentration-dependent manner.[7] The most important plasma binding proteins is albumin.[Label]

Metabolism

Mainly hepatically metabolized by CYP3A. 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.[1]

Route of elimination

Excreted fecally (85%, 25% as unchanged drug) and urine (6%, < 1% as unchanged drug).[Label]

Half life

Plasma drug elimination is really slow, giving rilpivirine a half-life of 34-55 hours after oral administration.[7]

Clearance

In HIV-1 patients, the apparent oral clearance is estimated to be 10.5-11.8 L/h.[12]

Toxicity

Rilpivirine did not induce chromosomal damage in vivo. It did not show any effect on mating or fertility in animal studies. On the other hand, mice studies have result positive for the formation of hepatocellular neoplasms which can be rodent-specific.[Label]

Affected organisms
  • Humans and other mammals
  • Human Immunodeficiency Virus
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcetaminophenThe serum concentration of Rilpivirine can be decreased when it is combined with Acetaminophen.Approved
AcetazolamideThe serum concentration of Rilpivirine can be increased when it is combined with Acetazolamide.Approved, Vet Approved
Acetyl sulfisoxazoleThe serum concentration of Rilpivirine can be increased when it is combined with Acetyl sulfisoxazole.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Rilpivirine.Approved
AlclometasoneThe serum concentration of Rilpivirine can be decreased when it is combined with Alclometasone.Approved
AldesleukinThe serum concentration of Rilpivirine can be increased when it is combined with Aldesleukin.Approved
AlfentanilThe serum concentration of Alfentanil can be decreased when it is combined with Rilpivirine.Approved, Illicit
AlimemazineThe serum concentration of Rilpivirine can be decreased when it is combined with Alimemazine.Approved, Vet Approved
AlphacetylmethadolThe serum concentration of Alphacetylmethadol can be decreased when it is combined with Rilpivirine.Experimental, Illicit
AlphaprodineThe serum concentration of Alphaprodine can be decreased when it is combined with Rilpivirine.Illicit
AlprazolamThe serum concentration of Rilpivirine can be increased when it is combined with Alprazolam.Approved, Illicit, Investigational
Aluminum hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Aluminum hydroxide.Approved, Investigational
AmbroxolThe serum concentration of Rilpivirine can be increased when it is combined with Ambroxol.Approved, Investigational
AminoglutethimideThe serum concentration of Rilpivirine can be decreased when it is combined with Aminoglutethimide.Approved, Investigational
AmiodaroneThe serum concentration of Rilpivirine can be increased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Rilpivirine can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Rilpivirine can be increased when it is combined with Amprenavir.Approved, Investigational
AnagrelideRilpivirine may increase the QTc-prolonging activities of Anagrelide.Approved
AnastrozoleThe serum concentration of Rilpivirine can be increased when it is combined with Anastrozole.Approved, Investigational
AntipyrineThe serum concentration of Rilpivirine can be increased when it is combined with Antipyrine.Approved, Investigational
ApalutamideThe serum concentration of Rilpivirine can be decreased when it is combined with Apalutamide.Approved, Investigational
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
ArmodafinilThe serum concentration of Rilpivirine can be decreased when it is combined with Armodafinil.Approved, Investigational
Arsenic trioxideThe serum concentration of Rilpivirine can be increased when it is combined with Arsenic trioxide.Approved, Investigational
ArtemetherThe serum concentration of Rilpivirine can be decreased when it is combined with Artemether.Approved
AsenapineRilpivirine may increase the QTc-prolonging activities of Asenapine.Approved
AstemizoleThe serum concentration of Rilpivirine can be increased when it is combined with Astemizole.Approved, Withdrawn
AsunaprevirThe serum concentration of Asunaprevir can be decreased when it is combined with Rilpivirine.Approved, Investigational, Withdrawn
AtazanavirThe serum concentration of Rilpivirine can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Rilpivirine can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Rilpivirine.Approved
AvasimibeThe serum concentration of Rilpivirine can be decreased when it is combined with Avasimibe.Investigational
AzatadineThe serum concentration of Rilpivirine can be decreased when it is combined with Azatadine.Approved
AzelastineThe serum concentration of Rilpivirine can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Azithromycin.Approved
Beclomethasone dipropionateThe serum concentration of Rilpivirine can be decreased when it is combined with Beclomethasone dipropionate.Approved, Investigational
BedaquilineRilpivirine may increase the QTc-prolonging activities of Bedaquiline.Approved
BetamethasoneThe serum concentration of Rilpivirine can be increased when it is combined with Betamethasone.Approved, Vet Approved
BexaroteneThe serum concentration of Rilpivirine can be decreased when it is combined with Bexarotene.Approved, Investigational
BicalutamideThe serum concentration of Rilpivirine can be increased when it is combined with Bicalutamide.Approved
BifonazoleThe serum concentration of Rilpivirine can be increased when it is combined with Bifonazole.Approved, Investigational
BoceprevirThe serum concentration of Rilpivirine can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe serum concentration of Rilpivirine can be increased when it is 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, Investigational
BrigatinibThe serum concentration of Rilpivirine can be decreased when it is combined with Brigatinib.Approved, Investigational
BromocriptineThe serum concentration of Rilpivirine can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Buprenorphine can be decreased when it is combined with Rilpivirine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe serum concentration of Butorphanol can be decreased when it is combined with Rilpivirine.Approved, Illicit, Vet Approved
CabergolineThe serum concentration of Rilpivirine can be increased when it is combined with Cabergoline.Approved
CaffeineThe serum concentration of Rilpivirine can be increased when it is combined with Caffeine.Approved
CalcitriolThe serum concentration of Rilpivirine can be decreased when it is combined with Calcitriol.Approved, Nutraceutical
Calcium CarbonateThe serum concentration of Rilpivirine can be decreased when it is combined with Calcium Carbonate.Approved, Investigational
CapsaicinThe serum concentration of Rilpivirine can be increased when it is combined with Capsaicin.Approved
CarbamazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarfentanilThe serum concentration of Carfentanil can be decreased when it is combined with Rilpivirine.Illicit, Investigational, Vet Approved
CaspofunginThe serum concentration of Rilpivirine can be increased when it is combined with Caspofungin.Approved
CefradineThe serum concentration of Rilpivirine can be decreased when it is combined with Cefradine.Approved
CeritinibThe serum concentration of Rilpivirine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Rilpivirine can be decreased when it is combined with Cerivastatin.Approved, Withdrawn
ChloramphenicolThe serum concentration of Rilpivirine can be increased when it is combined with Chloramphenicol.Approved, Vet Approved
ChloroquineRilpivirine may increase the QTc-prolonging activities of Chloroquine.Approved, Investigational, Vet Approved
ChlorphenesinThe serum concentration of Rilpivirine can be decreased when it is combined with Chlorphenesin.Approved, Vet Approved, Withdrawn
ChlorpromazineRilpivirine may increase the QTc-prolonging activities of Chlorpromazine.Approved, Investigational, Vet Approved
ChlorzoxazoneThe serum concentration of Rilpivirine can be increased when it is combined with Chlorzoxazone.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Rilpivirine.Approved, Investigational
CimetidineThe serum concentration of Rilpivirine can be decreased when it is combined with Cimetidine.Approved, Investigational
Cimicifuga racemosaThe serum concentration of Rilpivirine can be increased when it is combined with Cimicifuga racemosa.Approved, Experimental
CiprofloxacinThe serum concentration of Rilpivirine can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Rilpivirine can be increased when it is combined with Cisapride.Approved, Investigational, Withdrawn
CitalopramRilpivirine may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe serum concentration of Rilpivirine can be decreased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Rilpivirine can be increased when it is combined with Clemastine.Approved, Investigational
ClevidipineThe serum concentration of Rilpivirine can be decreased when it is combined with Clevidipine.Approved, Investigational
ClindamycinThe serum concentration of Rilpivirine can be increased when it is combined with Clindamycin.Approved, Vet Approved
ClobazamThe serum concentration of Rilpivirine can be decreased when it is combined with Clobazam.Approved, Illicit
ClofazimineThe serum concentration of Rilpivirine can be increased when it is combined with Clofazimine.Approved, Investigational
ClofibrateThe serum concentration of Rilpivirine can be decreased when it is combined with Clofibrate.Approved, Investigational
ClomifeneThe serum concentration of Rilpivirine can be increased when it is combined with Clomifene.Approved, Investigational
ClotiazepamThe serum concentration of Rilpivirine can be increased when it is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Rilpivirine can be decreased when it is combined with Clozapine.Approved
CobicistatThe serum concentration of Rilpivirine can be increased when it is combined with Cobicistat.Approved
CocaineThe serum concentration of Rilpivirine can be increased when it is combined with Cocaine.Approved, Illicit
CodeineThe serum concentration of Codeine can be decreased when it is combined with Rilpivirine.Approved, Illicit
ColchicineThe serum concentration of Rilpivirine can be decreased when it is combined with Colchicine.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Rilpivirine.Approved, Investigational
Cortisone acetateThe serum concentration of Rilpivirine can be increased when it is combined with Cortisone acetate.Approved, Investigational
CrizotinibThe serum concentration of Rilpivirine can be increased when it is combined with Crizotinib.Approved
CurcuminThe serum concentration of Rilpivirine can be increased when it is combined with Curcumin.Approved, Investigational
CyclophosphamideThe serum concentration of Rilpivirine can be decreased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Rilpivirine can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Rilpivirine.Approved
DabrafenibThe serum concentration of Rilpivirine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DalfopristinThe serum concentration of Rilpivirine can be increased when it is combined with Dalfopristin.Approved
DanazolThe serum concentration of Rilpivirine can be increased when it is combined with Danazol.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 Rilpivirine can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Rilpivirine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelafloxacinThe serum concentration of Rilpivirine can be decreased when it is combined with Delafloxacin.Approved, Investigational
DelavirdineThe serum concentration of Rilpivirine can be increased when it is combined with Delavirdine.Approved
DesipramineThe serum concentration of Rilpivirine can be increased when it is combined with Desipramine.Approved, Investigational
DesvenlafaxineThe serum concentration of Rilpivirine can be decreased when it is combined with Desvenlafaxine.Approved, Investigational
DexamethasoneThe serum concentration of Rilpivirine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Dextromethorphan can be decreased when it is combined with Rilpivirine.Approved
DextromoramideThe serum concentration of Dextromoramide can be decreased when it is combined with Rilpivirine.Experimental, Illicit
DextropropoxypheneThe serum concentration of Rilpivirine can be decreased when it is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe serum concentration of Dezocine can be decreased when it is combined with Rilpivirine.Approved, Investigational
DiacereinThe serum concentration of Rilpivirine can be increased when it is combined with Diacerein.Approved, Investigational
DiazepamThe serum concentration of Rilpivirine can be increased when it is combined with Diazepam.Approved, Illicit, Investigational, Vet Approved
DicloxacillinThe serum concentration of Rilpivirine can be decreased when it is combined with Dicloxacillin.Approved, Investigational, Vet Approved
DidanosineThe serum concentration of Didanosine can be increased when it is combined with Rilpivirine.Approved
DiethylstilbestrolThe serum concentration of Rilpivirine can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DihydrocodeineThe serum concentration of Dihydrocodeine can be decreased when it is combined with Rilpivirine.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Rilpivirine.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Rilpivirine.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Rilpivirine.Experimental
DihydroergotamineThe serum concentration of Rilpivirine can be increased when it is combined with Dihydroergotamine.Approved, Investigational
DihydroetorphineThe serum concentration of Dihydroetorphine can be decreased when it is combined with Rilpivirine.Experimental, Illicit
DihydromorphineThe serum concentration of Dihydromorphine can be decreased when it is combined with Rilpivirine.Experimental, Illicit
DiltiazemThe serum concentration of Rilpivirine can be increased when it is combined with Diltiazem.Approved, Investigational
Dimethyl sulfoxideThe serum concentration of Rilpivirine can be increased when it is combined with Dimethyl sulfoxide.Approved, Vet Approved
DiphenoxylateThe serum concentration of Diphenoxylate can be decreased when it is combined with Rilpivirine.Approved, Illicit
DisopyramideRilpivirine may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe serum concentration of Rilpivirine can be increased when it is combined with Docetaxel.Approved, Investigational
DofetilideRilpivirine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DolasetronRilpivirine may increase the QTc-prolonging activities of Dolasetron.Approved, Investigational
DomperidoneRilpivirine may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Rilpivirine.Approved, Investigational
DoxycyclineThe serum concentration of Rilpivirine can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe serum concentration of DPDPE can be decreased when it is combined with Rilpivirine.Experimental
DronedaroneThe serum concentration of Rilpivirine can be increased when it is combined with Dronedarone.Approved
DroperidolRilpivirine may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DrospirenoneThe serum concentration of Rilpivirine can be decreased when it is combined with Drospirenone.Approved
DrotebanolThe serum concentration of Drotebanol can be decreased when it is combined with Rilpivirine.Experimental, Illicit
EcgonineThe serum concentration of Ecgonine can be decreased when it is combined with Rilpivirine.Experimental, Illicit
EconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Econazole.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Rilpivirine.Approved
EfavirenzThe serum concentration of Rilpivirine can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipineThe serum concentration of Rilpivirine can be increased when it is combined with Efonidipine.Approved, Investigational
ElbasvirThe serum concentration of Rilpivirine can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Rilpivirine can be decreased when it is combined with Eletriptan.Approved, Investigational
EliglustatRilpivirine may increase the QTc-prolonging activities of Eliglustat.Approved
EnasidenibThe serum concentration of Rilpivirine can be decreased when it is combined with Enasidenib.Approved, Investigational
EnzalutamideThe serum concentration of Rilpivirine can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe serum concentration of Rilpivirine can be increased when it is combined with Epinephrine.Approved, Vet Approved
ErgonovineThe serum concentration of Rilpivirine can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Rilpivirine can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Rilpivirine can be increased when it is combined with Erythromycin.Approved, Investigational, 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 Rilpivirine can be decreased when it is combined with Estradiol.Approved, Investigational, Vet Approved
Estradiol acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Estradiol acetate.Approved, Investigational, Vet Approved
Estradiol benzoateThe serum concentration of Rilpivirine can be decreased when it is combined with Estradiol benzoate.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Rilpivirine can be decreased when it is combined with Estradiol cypionate.Approved, Investigational, Vet Approved
Estradiol dienanthateThe serum concentration of Rilpivirine can be decreased when it is combined with Estradiol dienanthate.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Rilpivirine can be decreased when it is combined with Estradiol valerate.Approved, Investigational, Vet Approved
EthanolThe serum concentration of Rilpivirine can be decreased when it is combined with Ethanol.Approved
EthylmorphineThe serum concentration of Ethylmorphine can be decreased when it is combined with Rilpivirine.Approved, Illicit
EtoposideThe serum concentration of Rilpivirine can be decreased when it is combined with Etoposide.Approved
EtoricoxibThe serum concentration of Rilpivirine can be increased when it is combined with Etoricoxib.Approved, Investigational
EtorphineThe serum concentration of Etorphine can be decreased when it is combined with Rilpivirine.Illicit, Vet Approved
EtravirineThe serum concentration of Rilpivirine can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Rilpivirine.Approved
ExemestaneThe serum concentration of Rilpivirine can be decreased when it is combined with Exemestane.Approved, Investigational
EzetimibeThe serum concentration of Rilpivirine can be increased when it is combined with Ezetimibe.Approved
FamotidineThe serum concentration of Rilpivirine can be decreased when it is combined with Famotidine.Approved
FelbamateThe serum concentration of Rilpivirine can be decreased when it is combined with Felbamate.Approved
FelodipineThe serum concentration of Rilpivirine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Rilpivirine.Approved, Illicit, Investigational, Vet Approved
FlecainideRilpivirine may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FlucloxacillinThe serum concentration of Rilpivirine can be decreased when it is combined with Flucloxacillin.Approved, Investigational
FluconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Fluconazole.Approved, Investigational
FluorometholoneThe serum concentration of Rilpivirine can be decreased when it is combined with Fluorometholone.Approved, Investigational
FluoxetineThe serum concentration of Rilpivirine can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolRilpivirine may increase the QTc-prolonging activities of Flupentixol.Approved, Investigational, Withdrawn
Fluticasone propionateThe serum concentration of Rilpivirine can be increased when it is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Rilpivirine can be decreased when it is combined with Fluvastatin.Approved
FluvoxamineThe serum concentration of Rilpivirine can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Rilpivirine can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rilpivirine can be decreased when it is combined with Fosaprepitant.Approved
FosnetupitantThe serum concentration of Rilpivirine can be increased when it is combined with Fosnetupitant.Approved
FosphenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Rilpivirine can be increased when it is combined with Fusidic Acid.Approved, Investigational
Gadobenic acidRilpivirine may increase the QTc-prolonging activities of Gadobenic acid.Approved, Investigational
GemfibrozilThe serum concentration of Rilpivirine can be decreased when it is combined with Gemfibrozil.Approved
GemifloxacinRilpivirine may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GestodeneThe serum concentration of Rilpivirine can be increased when it is combined with Gestodene.Approved, Investigational
GlecaprevirThe serum concentration of Rilpivirine can be increased when it is combined with Glecaprevir.Approved, Investigational
GlyburideThe serum concentration of Rilpivirine can be increased when it is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe serum concentration of Rilpivirine can be increased when it is combined with Glycerol Phenylbutyrate.Approved
GoserelinRilpivirine may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronRilpivirine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GriseofulvinThe serum concentration of Rilpivirine can be decreased when it is combined with Griseofulvin.Approved, Investigational, Vet Approved
GuanethidineThe serum concentration of Rilpivirine can be decreased when it is combined with Guanethidine.Approved
HaloperidolThe serum concentration of Rilpivirine can be increased when it is combined with Haloperidol.Approved
HeroinThe serum concentration of Heroin can be decreased when it is combined with Rilpivirine.Approved, Illicit, Investigational
HistamineThe serum concentration of Rilpivirine can be increased when it is combined with Histamine.Approved, Investigational
HydralazineThe serum concentration of Rilpivirine can be increased when it is combined with Hydralazine.Approved
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Rilpivirine.Approved, Illicit
HydrocortamateThe serum concentration of Rilpivirine can be decreased when it is combined with Hydrocortamate.Approved
HydrocortisoneThe serum concentration of Rilpivirine can be decreased when it is combined with Hydrocortisone.Approved, Vet Approved
HydromorphoneThe serum concentration of Hydromorphone can be decreased when it is combined with Rilpivirine.Approved, Illicit
IbrutinibThe serum concentration of Ibrutinib 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
IfosfamideThe serum concentration of Rilpivirine can be decreased when it is combined with Ifosfamide.Approved
IloperidoneThe serum concentration of Rilpivirine can be increased when it is combined with Iloperidone.Approved
ImatinibThe serum concentration of Rilpivirine can be increased when it is combined with Imatinib.Approved
IndinavirThe serum concentration of Rilpivirine can be increased when it is combined with Indinavir.Approved
IndisulamThe serum concentration of Rilpivirine can be increased when it is combined with Indisulam.Investigational
IrbesartanThe serum concentration of Rilpivirine can be increased when it is combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of Rilpivirine can be increased when it is combined with Irinotecan.Approved, Investigational
IsavuconazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of Rilpivirine can be decreased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe serum concentration of Rilpivirine can be increased when it is combined with Isoniazid.Approved, Investigational
IsradipineThe serum concentration of Rilpivirine can be increased when it is combined with Isradipine.Approved, Investigational
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
JosamycinThe serum concentration of Rilpivirine can be increased when it is combined with Josamycin.Approved, Investigational
KetazolamThe serum concentration of Rilpivirine can be increased when it is combined with Ketazolam.Approved
KetobemidoneThe serum concentration of Ketobemidone can be decreased when it is combined with Rilpivirine.Approved, Investigational
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Rilpivirine.Approved, Investigational
LansoprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Rilpivirine can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Rilpivirine.Approved
LenvatinibRilpivirine may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
LercanidipineThe serum concentration of Rilpivirine can be increased when it is combined with Lercanidipine.Approved, Investigational
LetermovirThe serum concentration of Rilpivirine can be increased when it is combined with Letermovir.Approved, Investigational
LeuprolideRilpivirine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevofloxacinThe serum concentration of Rilpivirine can be increased when it is combined with Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe serum concentration of Levomethadyl Acetate can be decreased when it is combined with Rilpivirine.Approved, Investigational
LevorphanolThe serum concentration of Levorphanol can be decreased when it is combined with Rilpivirine.Approved
LevosalbutamolThe serum concentration of Rilpivirine can be increased when it is combined with Levosalbutamol.Approved, Investigational
LidocaineThe serum concentration of Rilpivirine can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Rilpivirine can be increased when it is combined with Linagliptin.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Rilpivirine.Approved, Investigational
LofentanilThe serum concentration of Lofentanil can be decreased when it is combined with Rilpivirine.Illicit
LomitapideThe serum concentration of Rilpivirine can be increased when it is combined with Lomitapide.Approved, Investigational
LomustineThe serum concentration of Rilpivirine can be increased when it is combined with Lomustine.Approved, Investigational
LopinavirThe serum concentration of Rilpivirine can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Rilpivirine can be decreased when it is combined with Loratadine.Approved, Investigational
LorpiprazoleThe serum concentration of Rilpivirine can be increased when it is combined with Lorpiprazole.Approved
LosartanThe serum concentration of Rilpivirine can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Rilpivirine can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Rilpivirine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe serum concentration of Rilpivirine can be decreased when it is combined with Lumefantrine.Approved
LurasidoneThe serum concentration of Rilpivirine can be increased when it is combined with Lurasidone.Approved, Investigational
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Rilpivirine.Illicit, Investigational, Withdrawn
Magnesium hydroxideThe serum concentration of Rilpivirine can be decreased when it is combined with Magnesium hydroxide.Approved, Investigational
ManidipineThe serum concentration of Rilpivirine can be increased when it is combined with Manidipine.Approved, Investigational
Medroxyprogesterone acetateThe serum concentration of Rilpivirine can be decreased when it is combined with Medroxyprogesterone acetate.Approved, Investigational
MefloquineThe serum concentration of Rilpivirine can be increased when it is combined with Mefloquine.Approved, Investigational
MeptazinolThe serum concentration of Meptazinol can be decreased when it is combined with Rilpivirine.Experimental
MequitazineThe serum concentration of Rilpivirine can be increased when it is combined with Mequitazine.Approved
MetamizoleThe serum concentration of Rilpivirine can be decreased when it is combined with Metamizole.Approved, Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Rilpivirine.Experimental
MethadoneThe serum concentration of Rilpivirine can be decreased when it is combined with Methadone.Approved
Methadyl AcetateThe serum concentration of Methadyl Acetate can be decreased when it is combined with Rilpivirine.Approved, Illicit
MethazolamideThe serum concentration of Rilpivirine can be increased when it is combined with Methazolamide.Approved
MethimazoleThe serum concentration of Rilpivirine can be increased when it is combined with Methimazole.Approved
MethylecgonineThe serum concentration of Methylecgonine can be decreased when it is combined with Rilpivirine.Experimental
MethylergometrineThe serum concentration of Rilpivirine can be increased when it is combined with Methylergometrine.Approved
MethylprednisoloneThe serum concentration of Rilpivirine can be increased when it is combined with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Rilpivirine.Approved
MetronidazoleThe serum concentration of Rilpivirine can be increased when it is combined with Metronidazole.Approved
MetyraponeThe serum concentration of Rilpivirine can be decreased when it is combined with Metyrapone.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Rilpivirine.Experimental
MibefradilThe serum concentration of Rilpivirine can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Rilpivirine can be increased when it is combined with Midazolam.Approved, Illicit
MidostaurinThe serum concentration of Rilpivirine can be decreased when it is combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Rilpivirine can be decreased when it is combined with Mifepristone.Approved, Investigational
MirtazapineThe serum concentration of Rilpivirine can be increased when it is combined with Mirtazapine.Approved
MitotaneThe serum concentration of Rilpivirine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Rilpivirine can be increased when it is combined with Mitoxantrone.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 decreased when it is combined with Rilpivirine.Approved, Investigational
MoxifloxacinRilpivirine may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
MyrrhThe serum concentration of Rilpivirine can be decreased when it is combined with Myrrh.Approved
NabiloneThe serum concentration of Rilpivirine can be increased when it is combined with Nabilone.Approved, Investigational
NafcillinThe serum concentration of Rilpivirine can be decreased when it is combined with Nafcillin.Approved, Investigational
NalbuphineThe serum concentration of Nalbuphine can be decreased when it is combined with Rilpivirine.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Rilpivirine.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, Investigational
NevirapineThe serum concentration of Rilpivirine can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Rilpivirine can be decreased when it is combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Rilpivirine.Approved, Investigational
NicotinamideThe serum concentration of Rilpivirine can be increased when it is combined with Nicotinamide.Approved, Investigational
NifedipineThe serum concentration of Rilpivirine can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Rilpivirine can be increased when it is combined with Nilotinib.Approved, Investigational
NilvadipineThe serum concentration of Rilpivirine can be increased when it is combined with Nilvadipine.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Rilpivirine.Approved
NisoldipineThe serum concentration of Rilpivirine can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Rilpivirine can be increased when it is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe serum concentration of Rilpivirine can be increased when it is combined with Nitric Oxide.Approved
NizatidineThe serum concentration of Rilpivirine can be decreased when it is combined with Nizatidine.Approved
NorfloxacinThe serum concentration of Rilpivirine can be increased when it is combined with Norfloxacin.Approved
NorgestimateThe serum concentration of Rilpivirine can be decreased when it is combined with Norgestimate.Approved, Investigational
NormethadoneThe serum concentration of Normethadone can be decreased when it is combined with Rilpivirine.Approved, Illicit
NoscapineThe serum concentration of Rilpivirine can be increased when it is combined with Noscapine.Investigational
OfloxacinRilpivirine may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Rilpivirine can be increased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Rilpivirine can be increased when it is combined with Olaparib.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
OpiumThe serum concentration of Opium can be decreased when it is combined with Rilpivirine.Approved, Illicit
OritavancinThe serum concentration of Rilpivirine can be decreased when it is combined with Oritavancin.Approved, Investigational
OrlistatThe serum concentration of Rilpivirine can be decreased when it is combined with Orlistat.Approved, Investigational
OsimertinibThe serum concentration of Rilpivirine can be decreased when it is combined with Osimertinib.Approved
OxcarbazepineThe serum concentration of Rilpivirine can be decreased when it is combined with Oxcarbazepine.Approved
OxetacaineThe serum concentration of Rilpivirine can be increased when it is combined with Oxetacaine.Approved, Investigational
OxiconazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Oxiconazole.Approved
OxybutyninThe serum concentration of Rilpivirine can be increased when it is combined with Oxybutynin.Approved, Investigational
OxycodoneThe serum concentration of Oxycodone can be decreased when it is combined with Rilpivirine.Approved, Illicit, Investigational
OxymetholoneThe serum concentration of Rilpivirine can be increased when it is combined with Oxymetholone.Approved, Illicit
OxymorphoneThe serum concentration of Oxymorphone can be decreased when it is combined with Rilpivirine.Approved, Investigational, Vet Approved
PaclitaxelThe serum concentration of Rilpivirine can be decreased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Rilpivirine can be increased when it is combined with Palbociclib.Approved, Investigational
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
ParamethasoneThe serum concentration of Rilpivirine can be increased when it is combined with Paramethasone.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Rilpivirine.Approved
PegvisomantThe serum concentration of Rilpivirine can be decreased when it is combined with Pegvisomant.Approved
PentamidineRilpivirine may increase the QTc-prolonging activities of Pentamidine.Approved, Investigational
PentazocineThe serum concentration of Pentazocine can be decreased when it is combined with Rilpivirine.Approved, Vet Approved
PentobarbitalThe serum concentration of Rilpivirine can be decreased when it is combined with Pentobarbital.Approved, Investigational, Vet Approved
Peppermint oilThe serum concentration of Rilpivirine can be increased when it is combined with Peppermint oil.Approved, Investigational
PerampanelThe serum concentration of Rilpivirine can be decreased when it is combined with Perampanel.Approved
PerflutrenRilpivirine may increase the QTc-prolonging activities of Perflutren.Approved
PergolideThe serum concentration of Rilpivirine can be increased when it is combined with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PethidineThe serum concentration of Pethidine can be decreased when it is combined with Rilpivirine.Approved
PhenazocineThe serum concentration of Phenazocine can be decreased when it is combined with Rilpivirine.Experimental
PhenelzineThe serum concentration of Rilpivirine can be increased when it is combined with Phenelzine.Approved
PhenobarbitalThe serum concentration of Rilpivirine can be decreased when it is combined with Phenobarbital.Approved, Investigational
PhenoperidineThe serum concentration of Phenoperidine can be decreased when it is combined with Rilpivirine.Experimental
PhenylbutazoneThe serum concentration of Rilpivirine can be decreased when it is combined with Phenylbutazone.Approved, Vet Approved
PhenytoinThe serum concentration of Rilpivirine can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PibrentasvirThe serum concentration of Rilpivirine can be increased when it is combined with Pibrentasvir.Approved, Investigational
PilocarpineThe serum concentration of Rilpivirine can be increased when it is combined with Pilocarpine.Approved, Investigational
PimozideThe serum concentration of Rilpivirine can be increased when it is combined with Pimozide.Approved
PioglitazoneThe serum concentration of Rilpivirine can be decreased when it is combined with Pioglitazone.Approved, Investigational
PiperaquineThe serum concentration of Rilpivirine can be increased when it is combined with Piperaquine.Approved, Investigational
PiritramideThe serum concentration of Piritramide can be decreased when it is combined with Rilpivirine.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rilpivirine.Approved
PitolisantThe serum concentration of Rilpivirine can be decreased when it is combined with Pitolisant.Approved, Investigational
PosaconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrasteroneThe serum concentration of Rilpivirine can be increased when it is combined with Prasterone.Approved, Investigational, Nutraceutical
PravastatinThe serum concentration of Rilpivirine can be increased when it is combined with Pravastatin.Approved
PrednisoloneThe serum concentration of Rilpivirine can be increased when it is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Rilpivirine can be decreased when it is combined with Prednisone.Approved, Vet Approved
PrimaquineThe serum concentration of Rilpivirine can be increased when it is combined with Primaquine.Approved
PrimidoneThe serum concentration of Rilpivirine can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Rilpivirine can be decreased when it is combined with Probenecid.Approved, Investigational
ProcainamideRilpivirine may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Rilpivirine can be decreased when it is combined with Progesterone.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
PropofolThe serum concentration of Rilpivirine can be increased when it is combined with Propofol.Approved, Investigational, Vet Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Rilpivirine.Approved
PyridostigmineThe serum concentration of Rilpivirine can be decreased when it is combined with Pyridostigmine.Approved, Investigational
QuetiapineRilpivirine may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineThe serum concentration of Rilpivirine can be decreased when it is combined with Quinidine.Approved, Investigational
QuinineThe serum concentration of Rilpivirine can be decreased when it is combined with Quinine.Approved
QuinupristinThe serum concentration of Rilpivirine can be increased when it is combined with Quinupristin.Approved
RabeprazoleThe serum concentration of Rilpivirine can be decreased when it is combined with Rabeprazole.Approved, Investigational
RaloxifeneThe serum concentration of Rilpivirine can be increased when it is combined with Raloxifene.Approved, Investigational
RaltegravirThe serum concentration of Raltegravir can be increased when it is combined with Rilpivirine.Approved
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
RegorafenibThe serum concentration of Rilpivirine can be increased when it is combined with Regorafenib.Approved
RemifentanilThe serum concentration of Remifentanil can be decreased when it is combined with Rilpivirine.Approved
RepaglinideThe serum concentration of Rilpivirine can be increased when it is combined with Repaglinide.Approved, Investigational
ReserpineThe serum concentration of Rilpivirine can be decreased when it is combined with Reserpine.Approved, Investigational
ResveratrolThe serum concentration of Rilpivirine can be increased when it is combined with Resveratrol.Approved, Experimental, Investigational
RheinThe serum concentration of Rilpivirine can be increased when it is combined with Rhein.Experimental
RibociclibThe serum concentration of Rilpivirine can be increased when it is combined with Ribociclib.Approved, Investigational
RifabutinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifabutin.Approved, Investigational
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, Investigational
RifaximinThe serum concentration of Rilpivirine can be decreased when it is combined with Rifaximin.Approved, Investigational
RisperidoneThe serum concentration of Rilpivirine can be increased when it is combined with Risperidone.Approved, Investigational
RitonavirThe serum concentration of Rilpivirine can be decreased when it is combined with Ritonavir.Approved, Investigational
RivastigmineThe serum concentration of Rilpivirine can be increased when it is combined with Rivastigmine.Approved, Investigational
RofecoxibThe serum concentration of Rilpivirine can be decreased when it is combined with Rofecoxib.Approved, Investigational, Withdrawn
RolitetracyclineThe serum concentration of Rilpivirine can be increased when it is combined with Rolitetracycline.Approved
RosuvastatinThe serum concentration of Rilpivirine can be increased when it is combined with Rosuvastatin.Approved
RoxithromycinThe serum concentration of Rilpivirine can be increased when it is combined with Roxithromycin.Approved, Investigational, Withdrawn
RucaparibThe serum concentration of Rilpivirine can be increased when it is combined with Rucaparib.Approved, Investigational
RufinamideThe serum concentration of Rilpivirine can be decreased when it is combined with Rufinamide.Approved
RutinThe serum concentration of Rilpivirine can be increased when it is combined with Rutin.Experimental, Investigational
SalbutamolThe serum concentration of Rilpivirine can be increased when it is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe serum concentration of Rilpivirine can be increased when it is combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Rilpivirine can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Rilpivirine.Approved
SeproxetineThe serum concentration of Rilpivirine can be increased when it is combined with Seproxetine.Investigational
SeratrodastThe serum concentration of Rilpivirine can be decreased when it is combined with Seratrodast.Approved
SertralineThe serum concentration of Rilpivirine can be increased when it is combined with Sertraline.Approved
SildenafilThe serum concentration of Rilpivirine can be increased when it is 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, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Rilpivirine.Approved
SimvastatinThe serum concentration of Rilpivirine can be decreased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Rilpivirine can be increased when it is combined with Sirolimus.Approved, Investigational
SitaxentanThe serum concentration of Rilpivirine can be increased when it is combined with Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe serum concentration of Rilpivirine can be increased when it is combined with Sorafenib.Approved, Investigational
SotalolRilpivirine may increase the QTc-prolonging activities of Sotalol.Approved
St. John's WortThe serum concentration of Rilpivirine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Rilpivirine can be increased when it is combined with Stiripentol.Approved
SufentanilThe serum concentration of Sufentanil can be decreased when it is combined with Rilpivirine.Approved, Investigational
SulfamethoxazoleThe serum concentration of Rilpivirine can be increased when it is combined with Sulfamethoxazole.Approved
SulfanilamideThe serum concentration of Rilpivirine can be increased when it is combined with Sulfanilamide.Approved
SulfinpyrazoneThe serum concentration of Rilpivirine can be decreased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe serum concentration of Rilpivirine can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Rilpivirine can be increased when it is combined with Tacrolimus.Approved, Investigational
TadalafilThe serum concentration of Rilpivirine can be increased when it is combined with Tadalafil.Approved, Investigational
TamoxifenThe serum concentration of Rilpivirine can be decreased when it is combined with Tamoxifen.Approved
TapentadolThe serum concentration of Tapentadol can be decreased when it is combined with Rilpivirine.Approved
TelaprevirThe serum concentration of Rilpivirine can be increased when it is combined with Telaprevir.Approved, Withdrawn
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
TemozolomideThe serum concentration of Rilpivirine can be decreased when it is combined with Temozolomide.Approved, Investigational
TemsirolimusThe serum concentration of Rilpivirine can be increased when it is combined with Temsirolimus.Approved
TeniposideThe serum concentration of Rilpivirine can be increased when it is combined with Teniposide.Approved
Tenofovir disoproxilThe serum concentration of Tenofovir disoproxil can be increased when it is combined with Rilpivirine.Approved, Investigational
TerbinafineThe serum concentration of Rilpivirine can be decreased when it is combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Rilpivirine can be decreased when it is combined with Terfenadine.Approved, Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Rilpivirine.Experimental
TesmilifeneThe serum concentration of Rilpivirine can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Rilpivirine can be decreased when it is combined with Testosterone.Approved, Investigational
Testosterone cypionateThe serum concentration of Rilpivirine can be decreased when it is combined with Testosterone cypionate.Approved
Testosterone enanthateThe serum concentration of Rilpivirine can be decreased when it is combined with Testosterone enanthate.Approved
Testosterone undecanoateThe serum concentration of Rilpivirine can be decreased when it is combined with Testosterone undecanoate.Approved, Investigational
TetrabenazineRilpivirine may increase the QTc-prolonging activities of Tetrabenazine.Approved, Investigational
TetracyclineThe serum concentration of Rilpivirine can be increased when it is combined with Tetracycline.Approved, Vet Approved
ThalidomideThe serum concentration of Rilpivirine can be decreased when it is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiopentalThe serum concentration of Rilpivirine can be increased when it is combined with Thiopental.Approved, Vet Approved
ThioridazineRilpivirine may increase the QTc-prolonging activities of Thioridazine.Approved, Withdrawn
TicagrelorThe serum concentration of Rilpivirine can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe serum concentration of Rilpivirine can be increased when it is combined with Ticlopidine.Approved
TilidineThe serum concentration of Tilidine can be decreased when it is combined with Rilpivirine.Experimental
TioconazoleThe serum concentration of Rilpivirine can be increased when it is combined with Tioconazole.Approved
TipranavirThe serum concentration of Rilpivirine can be increased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Rilpivirine can be decreased when it is combined with Tocilizumab.Approved
TofisopamThe serum concentration of Rilpivirine can be increased when it is combined with Tofisopam.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Rilpivirine.Approved
TopiramateThe serum concentration of Rilpivirine can be decreased when it is combined with Topiramate.Approved
TopiroxostatThe serum concentration of Rilpivirine can be increased when it is combined with Topiroxostat.Approved, Investigational
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
TramadolThe serum concentration of Tramadol can be decreased when it is combined with Rilpivirine.Approved, Investigational
TrametinibThe serum concentration of Rilpivirine can be decreased when it is combined with Trametinib.Approved
TranylcypromineThe serum concentration of Rilpivirine can be increased when it is combined with Tranylcypromine.Approved, Investigational
TroglitazoneThe serum concentration of Rilpivirine can be decreased when it is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe serum concentration of Rilpivirine can be increased when it is combined with Troleandomycin.Approved
Valproic AcidThe serum concentration of Rilpivirine can be increased when it is combined with Valproic Acid.Approved, Investigational
VandetanibRilpivirine may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibThe serum concentration of Rilpivirine can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Rilpivirine can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Rilpivirine can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Rilpivirine can be increased when it is combined with Vinblastine.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Rilpivirine.Approved, Investigational
VincristineThe serum concentration of Rilpivirine can be increased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Rilpivirine can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Rilpivirine.Approved, Investigational
ZafirlukastThe serum concentration of Rilpivirine can be increased when it is combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe serum concentration of Rilpivirine can be increased when it is combined with Ziprasidone.Approved
ZucapsaicinThe serum concentration of Rilpivirine can be increased when it is combined with Zucapsaicin.Approved, Investigational
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

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. Putcharoen O, Kerr SJ, Ruxrungtham K: An update on clinical utility of rilpivirine in the management of HIV infection in treatment-naive patients. HIV AIDS (Auckl). 2013 Sep 16;5:231-41. doi: 10.2147/HIV.S25712. [PubMed:24068877]
  6. Usach I, Melis V, Peris JE: Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability. J Int AIDS Soc. 2013 Sep 4;16:1-14. doi: 10.7448/IAS.16.1.18567. [PubMed:24008177]
  7. Ford N, Lee J, Andrieux-Meyer I, Calmy A: Safety, efficacy, and pharmacokinetics of rilpivirine: systematic review with an emphasis on resource-limited settings. HIV AIDS (Auckl). 2011;3:35-44. doi: 10.2147/HIV.S14559. Epub 2011 Apr 28. [PubMed:22096405]
  8. Azijn H, Tirry I, Vingerhoets J, de Bethune MP, Kraus G, Boven K, Jochmans D, Van Craenenbroeck E, Picchio G, Rimsky LT: TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. doi: 10.1128/AAC.00986-09. Epub 2009 Nov 23. [PubMed:19933797]
  9. Lexicomp 2013 [Link]
  10. J&J News [Link]
  11. FDA News and Events [Link]
  12. Australian report [Link]
  13. J&J News [Link]
External Links
Human Metabolome Database
HMDB0061725
KEGG Drug
D09720
PubChem Compound
6451164
PubChem Substance
175427123
ChemSpider
4953643
BindingDB
222178
ChEBI
68606
ChEMBL
CHEMBL175691
HET
T27
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rilpivirine
ATC Codes
J05AR19 — Emtricitabine, tenofovir alafenamide and rilpivirineJ05AG05 — RilpivirineJ05AR08 — Emtricitabine, tenofovir disoproxil and rilpivirine
AHFS Codes
  • 08:18.08.16 — Nonnucleoside Reverse Transcriptase Inhibitors
PDB Entries
2zd1 / 2ze2 / 3bgr / 3mee / 3meg / 3qlh / 4g1q / 4icl / 4id5 / 4idk
show 7 more
FDA label
Download (558 KB)
MSDS
Download (568 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAcquired Immune Deficiency Syndrome (AIDS) / Hepatic Impairment / Human Immunodeficiency Virus (HIV)1
1CompletedNot AvailableHuman Immunodeficiency Virus (HIV)1
1CompletedNot AvailableInfections, Human Immunodeficiency Virus and Hepatitis1
1CompletedDiagnosticHuman Volunteers1
1CompletedOtherHIV-DDI1
1CompletedTreatmentAcquired Immune Deficiency Syndrome (AIDS) / Human Immunodeficiency Virus (HIV) / Oral Contraceptives (OC)1
1CompletedTreatmentBioavailability / Human Immunodeficiency Virus Type 1 (HIV-1) / Pharmacokinetics1
1CompletedTreatmentHealthy Participants1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV)1
1CompletedTreatmentHepatitis C Virus (HCV)1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV)2
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections2
1CompletedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1)1
1RecruitingOtherHealthy Volunteers1
1RecruitingTreatmentInsulin Resistance1
1TerminatedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1)1
1, 2Not Yet RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2TerminatedPreventionHuman Immunodeficiency Virus (HIV) Infections1
1, 2WithdrawnTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2CompletedPreventionHuman Immunodeficiency Virus (HIV)1
2CompletedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1)1
2CompletedTreatmentInfection, Human Immunodeficiency Virus I1
2RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
2RecruitingTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1)1
2, 3Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV)1
2, 3Enrolling by InvitationTreatmentHuman Immunodeficiency Virus (HIV)1
3Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections3
3Active Not RecruitingTreatmentHuman Immunodeficiency Virus-type 1 Infection1
3Active Not RecruitingTreatmentInfection, Human Immunodeficiency Virus I3
3CompletedTreatmentHCV Infections / Infection, Human Immunodeficiency Virus I1
3CompletedTreatmentHuman Immunodeficiency Virus (HIV)1
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Human Immunodeficiency Virus Type 1 (HIV-1)2
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections / Pregnancy1
3CompletedTreatmentInfection, Human Immunodeficiency Virus I3
3Not Yet RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
4Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV)1
4CompletedTreatmentCardiovascular Disease (CVD)1
4CompletedTreatmentHIV Associated Neurocognitive Disorders (HAND) / Neurocognitive Decline1
4CompletedTreatmentHealthy Volunteers2
4CompletedTreatmentHuman Immunodeficiency Virus (HIV)1
4CompletedTreatmentInfection, Human Immunodeficiency Virus I1
4Not Yet RecruitingTreatmentHiv-positive1
4RecruitingTreatmentAntiretroviral Therapy Intolerance / Patients Compliance1
4RecruitingTreatmentHIV-1-infection / Neurocognitive Dysfunction1
4TerminatedTreatmentHuman Immunodeficiency Virus (HIV)1
4WithdrawnNot AvailableHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
Not AvailableActive Not RecruitingTreatmentAnti-Retroviral Agents / Dyslipidemias / Efavirenz / HIV-1-infection / Rilpivirine / Sustained Virologic Response1
Not AvailableNot Yet RecruitingNot AvailableHuman Immunodeficiency Virus (HIV) Infections1
Not AvailableRecruitingNot AvailableMinor Patient Treated by One or More Antiretroviral and for Which a Blood Test Has Been Performed1
Not AvailableRecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
TabletOral25 mg
Tablet, film coatedOral25 mg
Tablet, film coatedOral25 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5914331Yes1998-01-022018-01-02Us
US6043230Yes1998-01-252018-01-25Us
US9242986No2009-10-082029-10-08Us
US5814639Yes1997-03-292017-03-29Us
US6642245Yes2001-05-042021-05-04Us
US6703396Yes2001-09-092021-09-09Us
US5922695Yes1998-01-252018-01-25Us
US5935946Yes1998-01-252018-01-25Us
US5977089Yes1998-01-252018-01-25Us
US8592397No2004-01-132024-01-13Us
US8716264No2004-01-132024-01-13Us
US7125879No2002-08-092022-08-09Us
US6838464No2001-02-262021-02-26Us
US8080551No2003-04-112023-04-11Us
US8101629No2002-08-092022-08-09Us
US7067522No1999-12-202019-12-20Us
US7638522No2003-04-142023-04-14Us
US8129385No2007-10-052027-10-05Us
US8841310No2005-12-092025-12-09Us
US9296769No2012-08-152032-08-15Us
US7803788No2002-02-022022-02-02Us
US8754065No2012-08-152032-08-15Us
US7390791No2002-05-072022-05-07Us
US9457036No2004-01-132024-01-13Us
US9744181No2004-01-132024-01-13Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)241-243°CSun, et al.: J. Med. Chem., 41, 4648 (1998) Kashiwada, et al.: Bioorg. Med. Chem. Lett., 11, 183 (2001)
water solubility<0.1mg/mlUsach, et al. J Int AIDS Soc. 16(1): 18567. (2013)
logP4.86Usach, et al. J Int AIDS Soc. 16(1): 18567. (2013)
pKa5.6Usach, et al. J Int AIDS Soc. 16(1): 18567. (2013)
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 FiveNoChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzonitriles. These are organic compounds containing a benzene bearing a nitrile substituent.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzonitriles
Direct Parent
Benzonitriles
Alternative Parents
m-Xylenes / Styrenes / Aniline and substituted anilines / Aminopyrimidines and derivatives / Imidolactams / Hydropyrimidines / Heteroaromatic compounds / Secondary amines / Nitriles / Azacyclic compounds
show 2 more
Substituents
Benzonitrile / M-xylene / Xylene / Styrene / Aniline or substituted anilines / Aminopyrimidine / Hydropyrimidine / Pyrimidine / Imidolactam / Heteroaromatic compound
show 11 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aminopyrimidine, nitrile (CHEBI:68606)

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
Uniprot Name
Reverse transcriptase/RNaseH
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 an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
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
Substrate
Inhibitor
Inducer
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Other/unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

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
Uniprot Name
Multidrug resistance protein 1
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
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, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
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), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
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]

Drug created on March 14, 2013 15:23 / Updated on July 16, 2018 21:25