About: Rilpivirine     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/description
  • Rilpivirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) which is used for the treatment of HIV-1 infections in treatment-naive patients. It is a diarylpyrimidine, a class of molecules that resemble pyrimidine nucleotides found in DNA. Because of its flexible chemical structure, resistance of rilpivirine is less likely to develop than other NNRTI's. FDA approved on May 20, 2011. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # 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":http://www.ncbi.nlm.nih.gov/pubmed/19548857 # "Lexicomp 2013":http://lexicomp.com # 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":http://www.ncbi.nlm.nih.gov/pubmed/22519768 # 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":http://www.ncbi.nlm.nih.gov/pubmed/23428312 # 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":http://www.ncbi.nlm.nih.gov/pubmed/23157601 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 34-55 hours after oral administration (en)
http://linked.open...ugbank/indication
  • Treatment of HIV-1 infections in treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL in combination with at least 2 other antiretroviral agents. (en)
sameAs
Title
  • Rilpivirine (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Rilpivirine is an NNRTI which binds to reverse transcriptase which results in a block in RNA and DNA- dependent DNA polymerase activities. One such activity is HIV-1 replication. Intracellular phosphorylation is not necessary for its antiviral activity. Because of the structure of rilpivirine is flexible around the aromatic rings, the molecule can have multiple conformations so that can bind to residues in the reverse transcriptase enzyme which have a lower mutation rate. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Excreted fecally (85%, 25% as unchanged drug) and urine (6%, <1% as unchanged drug) (en)
http://linked.open.../drugbank/synonym
  • TMC278 (en)
  • TMC 278 (en)
  • 4-{[4-({4-[(e)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile (en)
http://linked.open...drugbank/toxicity
  • Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Co-administration with St. John's wort decreases levels of rilpivirine by inducing CYP3A4 metabolism. Use is contraindicated. (en)
  • Absorption is increased by 40% if taken with food. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • >99% protein bound. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Rilpivirine demonstrates dose-dependent pharmacokinetics and does not change between subscutaneous, IV, and intramuscular administration. Absorption increases with meals. Tmax, oral administration = 4 hours; (en)
http://linked.open.../affectedOrganism
  • Human Immunodeficiency Virus (en)
http://linked.open...casRegistryNumber
  • 500287-72-9 (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...ank/Melting-Point
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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