Source:http://linkedlifedata.com/resource/pubmed/id/11569933
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2001-9-24
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pubmed:abstractText |
Bristol-Myers Squibb (BMS) is developing entecavir, a viral replication inhibitor, for the potential treatment of hepatitis B virus (HBV) infection [220240]. The compound is a cyclopentyl guanosine analog and is in phase II trials in the US [383065]. Entecavir was originally developed as SQ-34676 for the treatment of herpes simplex virus infections [221992], but displayed only moderate activity which eventually led to discontinuation of development for this indication. However, Bristol-Myers Squibb later discovered that entecavir was extremely potent against HBV (ED50 = 3.0 nM, compared with 200 nM for lamivudine) with relatively low toxicity (CC50 = 30,000 nM) [221986] and acted through inhibition of DNA polymerase [220240]. The triphosphate form is a potent HBV polymerase inhibitor in both woodchuck and duck models [306056]. By September 2000, a large-scale clinical trial was underway in China for HBV infection [400209] and by October 2000 phase I trials were ongoing in Japan [384751]. In March 2001 SG Cowen predicted sales of US$25 million in 2002, US$50 million in 2003 and US$75 million in 2004 [403751].
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Directed DNA Polymerase,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Guanine,
http://linkedlifedata.com/resource/pubmed/chemical/entecavir
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1472-4472
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
2
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
617-21
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:11569933-Animals,
pubmed-meshheading:11569933-Antiviral Agents,
pubmed-meshheading:11569933-Clinical Trials as Topic,
pubmed-meshheading:11569933-DNA-Directed DNA Polymerase,
pubmed-meshheading:11569933-Enzyme Inhibitors,
pubmed-meshheading:11569933-Guanine,
pubmed-meshheading:11569933-Hepatitis B,
pubmed-meshheading:11569933-Herpes Simplex,
pubmed-meshheading:11569933-Humans,
pubmed-meshheading:11569933-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
Entecavir (Bristol-Myers Squibb).
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pubmed:affiliation |
Novartis Research Institute, General Dermatology, Vienna, Austria. andreas.billich@pharma.novartis.com
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pubmed:publicationType |
Journal Article,
Review
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