About: Tipranavir     Goto   Sponge   NotDistinct   Permalink

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

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http://linked.open...gbank/description
  • Tipranavir is a sulfonamide-containing dyhydropyrone and a nonpeptidic protease inhibitor that targets the HIV protease. It is administered with ritonavir in combination therapy to treat HIV infections. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Doyon L, Tremblay S, Bourgon L, Wardrop E, Cordingley MG: Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir. Antiviral Res. 2005 Oct;68(1):27-35. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16122817 # Tipranavir: PNU 140690, tipranivir. Drugs R D. 2006;7(1):55-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16620137 # Temesgen Z, Feinberg J: Tipranavir: a new option for the treatment of drug-resistant HIV infection. Clin Infect Dis. 2007 Sep 15;45(6):761-9. Epub 2007 Aug 7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17712762 # Luna B, Townsend MU: Tipranavir: the first nonpeptidic protease inhibitor for the treatment of protease resistance. Clin Ther. 2007 Nov;29(11):2309-18. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18158073 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 5-6 hours (en)
http://linked.open...ugbank/indication
  • For combination antiretroviral treatment of HIV-1 infected adult patients with evidence of viral replication, who are highly treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Tipranavir (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Tipranavir (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions. Two mechanisms are suggested in regards to the potency of tipranavir: 1. Tipravanir may bind to the active site of the protease enzyme with fewer hydrogen bonds than peptidic protease inhibitors, which results in increased flexibility, allowing it to fit into the active site of the enzyme in viruses that have become resistance to other protease inhibitors. This also enables tipranavir to adjust to amino acid substitutions at the active site. 2. Tipranavir's strong hydrogen bonding interaction with the amide backbone of the protease active site Asp30 may lead to its activity against resistant viruses. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open.../drugbank/synonym
  • TPV (en)
http://linked.open...drugbank/toxicity
  • Oral LD<sub>50</sub> in rat is over 5,000 mg/kg. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • Extensive (> 99.9%), to both human serum albumin and &alpha;-1-acid glycoprotein. (en)
http://linked.open...ynthesisReference
  • Franz Klingler, "Enantioselective hydrogenation of intermediates in the synthesis of tipranavir." U.S. Patent US20040224990, issued November 11, 2004. (en)
http://linked.open...y/mesh/hasConcept
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
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http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Absorption is limited, although no absolute quantification of absorption is available. (en)
http://linked.open.../affectedOrganism
  • Human Immunodeficiency Virus (en)
http://linked.open...casRegistryNumber
  • 174484-41-4 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...gbank/containedIn
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http://linked.open...nk/MDDR-Like-Rule
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http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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