Identification

Name
Rilpivirine
Accession Number
DB08864
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

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 366.4185
Monoisotopic: 366.159294606
Chemical Formula
C22H18N6
Synonyms
  • 4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
  • Rilpivirina
  • Rilpivirine
External IDs
  • R 278474
  • R-278474
  • TMC 278
  • TMC-278
  • TMC278

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
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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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
Humans
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

Hover over products below to view reaction partners

Route of elimination

Excreted fecally (85%, 25% as unchanged drug) and urine (6%, < 1% as unchanged drug).Label,12

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

Adverse Effects
Learn about our commercial Adverse Effects data.
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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
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Rilpivirine can be increased when it is combined with Abametapir.
AbemaciclibRilpivirine may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Rilpivirine.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Rilpivirine.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Rilpivirine.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Rilpivirine.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Rilpivirine.
AcrivastineThe risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Rilpivirine is combined with Adenosine.
Adenovirus type 7 vaccine liveThe therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Rilpivirine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid St. John's Wort. St.John's Wort will decrease levels of this medication.
  • Take with food. Absorption is increased by 40% if taken with food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Rilpivirine hydrochloride212WAX8KDD700361-47-3KZVVGZKAVZUACK-BJILWQEISA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EdurantTablet25 mgOralJanssen Pharmaceuticals2011-08-31Not applicableCanada flag
EdurantTablet, film coated25 mg/1OralJanssen Products, LP2011-05-20Not applicableUS flag
EdurantTablet, film coated25 mgOralJanssen Cilag International Nv2011-11-28Not applicableEU flag
OdefseyTablet, film coatedOralGilead Sciences Ireland Uc2016-06-21Not applicableEU flag
OdefseyTablet, film coatedOralGilead Sciences Ireland Uc2016-06-21Not applicableEU flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CabenuvaRilpivirine (300 mg) + Cabotegravir (200 mg)Kit; Suspension, extended releaseIntramuscularViiV Healthcare ULC2020-09-21Not applicableCanada flag
CabenuvaRilpivirine (300 mg) + Cabotegravir (200 mg)Kit; Suspension, extended releaseIntramuscularViiV Healthcare ULC2020-09-21Not applicableCanada flag
CompleraRilpivirine hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralREMEDYREPACK INC.2017-08-162020-05-01US flag
CompleraRilpivirine hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralGilead Sciences, Inc.2011-08-10Not applicableUS flag
CompleraRilpivirine hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralA-S Medication Solutions2011-08-10Not applicableUS flag
CompleraRilpivirine hydrochloride (25 mg/1) + Emtricitabine (200 mg/1) + Tenofovir disoproxil fumarate (300 mg/1)Tablet, film coatedOralA-S Medication Solutions2011-08-102019-01-31US flag
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 flag
CompleraRilpivirine (25 mg) + Emtricitabine (200 mg) + Tenofovir disoproxil fumarate (300 mg)TabletOralGilead Sciences2011-10-20Not applicableCanada flag
JulucaRilpivirine (25 mg) + Dolutegravir (50 mg)TabletOralViiV Healthcare ULC2018-06-04Not applicableCanada flag
JulucaRilpivirine hydrochloride (25 mg/1) + Dolutegravir Sodium (50 mg/1)Tablet, film coatedOralViiV Healthcare Company2017-11-21Not applicableUS flag

Categories

ATC Codes
J05AR19 — Emtricitabine, tenofovir alafenamide and rilpivirineJ05AR21 — Dolutegravir and rilpivirineJ05AR08 — Emtricitabine, tenofovir disoproxil and rilpivirineJ05AG05 — Rilpivirine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Amine / Aminopyrimidine / Aniline or substituted anilines / Aromatic heteromonocyclic compound / Azacycle / Benzonitrile / Carbonitrile / Heteroaromatic compound / Hydrocarbon derivative / Hydropyrimidine
show 11 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aminopyrimidine, nitrile (CHEBI:68606)

Chemical Identifiers

UNII
FI96A8X663
CAS number
500287-72-9
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

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]
Human Metabolome Database
HMDB0061725
KEGG Drug
D09720
PubChem Compound
6451164
PubChem Substance
175427123
ChemSpider
4953643
BindingDB
222178
RxNav
1102270
ChEBI
68606
ChEMBL
CHEMBL175691
ZINC
ZINC000001554274
PDBe Ligand
T27
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
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
4Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
4CompletedPreventionHIV Nonoccupational Post-exposure Prophylaxis in Men Who Have Sex With Men1
4CompletedTreatmentCardiovascular Heart Disease1
4CompletedTreatmentDepression/Anxiety / Human Immunodeficiency Virus Type 1 (HIV-1) Infection / Impaired Cognition / Poor Quality Sleep / Quality of Life1
4CompletedTreatmentHealthy Volunteers2
4CompletedTreatmentHIV Associated Neurocognitive Disorders (HAND) / HIV-Associated neurocognitive disorder (HAND) / Neurocognitive Decline1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections2
4CompletedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1)1
4CompletedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
4Enrolling by InvitationTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection / Neurocognitive Dysfunction1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Kit; suspension, extended releaseIntramuscular
Tablet, film coatedOral
Tablet25 mg
TabletOral25 mg
Tablet, coatedOral25 mg
Tablet, film coatedOral25 mg
Tablet, film coatedOral25 mg/1
Tablet, coated25 mg
Tablet
Tablet, film coatedOral200 mg
Tablet, film coatedOral50 MG
TabletOral
TabletOral200 MG
Tablet, film coatedOral
Tablet, coatedOral200 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5914331Yes1999-06-222018-01-02US flag
US6043230Yes2000-03-282018-01-25US flag
US9242986No2016-01-262029-10-08US flag
US5814639Yes1998-09-292017-03-29US flag
US6642245Yes2003-11-042021-05-04US flag
US6703396Yes2004-03-092021-09-09US flag
US5922695Yes1999-07-132018-01-25US flag
US5935946Yes1999-08-102018-01-25US flag
US5977089Yes1999-11-022018-01-25US flag
US8592397No2013-11-262024-01-13US flag
US8716264No2014-05-062024-01-13US flag
US7125879No2006-10-242022-08-09US flag
US6838464No2005-01-042021-02-26US flag
US8080551No2011-12-202023-04-11US flag
US8101629No2012-01-242022-08-09US flag
US7067522No2006-06-272019-12-20US flag
US7638522No2009-12-292023-04-14US flag
US8129385No2012-03-062027-10-05US flag
US8841310No2014-09-232025-12-09US flag
US9296769No2016-03-292032-08-15US flag
US7803788No2010-09-282022-02-02US flag
US8754065No2014-06-172032-08-15US flag
US7390791No2008-06-242022-05-07US flag
US9457036No2016-10-042024-01-13US flag
US9744181No2017-08-292024-01-13US flag
US10426780No2019-10-012031-01-24US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

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)11.43ChemAxon
pKa (Strongest Basic)4.44ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area97.42 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity111.74 m3·mol-1ChemAxon
Polarizability40.63 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

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
Humans
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
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
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]
  2. Rilpivirine FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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]
  2. Aouri M, Barcelo C, Guidi M, Rotger M, Cavassini M, Hizrel C, Buclin T, Decosterd LA, Csajka C: Population Pharmacokinetics and Pharmacogenetics Analysis of Rilpivirine in HIV-1-Infected Individuals. Antimicrob Agents Chemother. 2016 Dec 27;61(1). pii: AAC.00899-16. doi: 10.1128/AAC.00899-16. Print 2017 Jan. [PubMed:27799217]
  3. Actual and Predicted Pharmacokinetic Interactions Between Anticonvulsants and Antiretrovirals [File]
Kind
Protein
Organism
Humans
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
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 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
Humans
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
Humans
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
Humans
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
Humans
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
Humans
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 October 21, 2020 01:55

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