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rdf:type
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http://linked.open...gbank/description
| - Brecanavir (VX-385) an orally active aspartic protease inhibitor (PI), under investigation by Vertex and GlaxoSmithKline for the treatment of HIV. In July 2006, Vertex indicated that it expected GSK to initiate phase III trials of the drug in 2007. In December of 2006 GSK announced a decision to discontinue the development of brecanavir for the treatment of HIV. The decision was based on issues regarding the formulation of the drug. (en)
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http://linked.open...generalReferences
| - # Hazen R, Harvey R, Ferris R, Craig C, Yates P, Griffin P, Miller J, Kaldor I, Ray J, Samano V, Furfine E, Spaltenstein A, Hale M, Tung R, St Clair M, Hanlon M, Boone L: In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. Antimicrob Agents Chemother. 2007 Sep;51(9):3147-54. Epub 2007 Jul 9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17620375 # Lalezari JP, Ward DJ, Tomkins SA, Garges HP: Preliminary safety and efficacy data of brecanavir, a novel HIV-1 protease inhibitor: 24 week data from study HPR10006. J Antimicrob Chemother. 2007 Jul;60(1):170-4. Epub 2007 May 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17491001 # Reddy YS, Ford SL, Anderson MT, Murray SC, Ng-Cashin J, Johnson MA: Safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus type 1 protease inhibitor, following repeat administration with and without ritonavir in healthy adult subjects. Antimicrob Agents Chemother. 2007 Apr;51(4):1202-8. Epub 2007 Jan 29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17261626 # Ford SL, Reddy YS, Anderson MT, Murray SC, Fernandez P, Stein DS, Johnson MA: Single-dose safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus protease inhibitor. Antimicrob Agents Chemother. 2006 Jun;50(6):2201-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16723584 (en)
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http://linked.open...gy/drugbank/group
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http://linked.open...ugbank/indication
| - For the treatment of HIV-1 infection in combination with other antiretroviral agents. (en)
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sameAs
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Title
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adms:identifier
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http://linked.open...mechanismOfAction
| - Brecanavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. (en)
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http://linked.open.../drugbank/synonym
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http://linked.open...nk/proteinBinding
| - Estimated be 97 to 98% (en)
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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...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...ugbank/absorption
| - Brecanavir, a CYP3A4 substrate, demonstrated low oral bioavailability in animals (0 to 30%), which increased to 60 to 100% following coadministration with oral ritonavir (a potent CYP3A inhibitor). (en)
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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...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...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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