| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Efavirenz (brand names Sustiva® and Stocrin®) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1. For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen. Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Ren J, Bird LE, Chamberlain PP, Stewart-Jones GB, Stuart DI, Stammers DK: Structure of HIV-2 reverse transcriptase at 2.35-A resolution and the mechanism of resistance to non-nucleoside inhibitors. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14410-5. Epub 2002 Oct 17. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12386343 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
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| http://linked.open...ugbank/indication
| - For use in combination treatment of HIV infection (AIDS) (en)
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| http://linked.open...bank/manufacturer
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Similar to zidovudine, efavirenz inhibits the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). Antiviral activity of efavirenz is dependent on intracellular conversion to the active triphosphorylated form. The rate of efavirenz phosphorylation varies, depending on cell type. It is believed that inhibition of reverse transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body. Even though human DNA polymerase is less susceptible to the pharmacologic effects of triphosphorylated efavirenz, this action may nevertheless account for some of the drug's toxicity. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Nearly all of the urinary excretion of the radiolabeled drug was in the form of metabolites. (en)
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| http://linked.open.../drugbank/synonym
| - Efavirenz (en)
- (S)-6-chloro-4-(Cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one (en)
- Efavirenzum (en)
- (-)-6-CHLORO-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one (en)
- 6-chloro-4-(2-Cyclopropyl-1-ethynyl)-4-trifluoromethyl-(4S)-1,4-dihydro-2H-benzo[D][1,3]oxazin-2-one (en)
- Éfavirenz (en)
- (S)-6-chloro-4-Cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[D][1,3]oxazin-2-one (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Avoid excessive or chronic alcohol consumption. (en)
- Take without regard to meals. (en)
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| http://linked.open...nk/proteinBinding
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| http://linked.open...ynthesisReference
| - John Doney, "Amorphous efavirenz and the production thereof." U.S. Patent US20070026073, issued February 01, 2007. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open.../affectedOrganism
| - Human Immunodeficiency Virus (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...gbank/containedIn
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...ank/Melting-Point
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
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