| pubmed-article:19894743 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0019196 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0034693 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0032105 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0022262 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0033607 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C0332157 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C2349975 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C1876229 | lld:lifeskim |
| pubmed-article:19894743 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:19894743 | pubmed:issue | 24 | lld:pubmed |
| pubmed-article:19894743 | pubmed:dateCreated | 2009-12-17 | lld:pubmed |
| pubmed-article:19894743 | pubmed:abstractText | Telaprevir 2 (VX-950), an inhibitor of the hepatitis C virus (HCV(a)) NS3-4A protease, is in phase 3 clinical trials. One of the major metabolites of 2 is its P1-(R)-diastereoisomer, 3 (VRT-394), containing an inversion at the chiral center next to the alpha-ketoamide on exchange of a proton with solvent. Compound 3 is approximately 30-fold less active against HCV protease. In an attempt to suppress the epimerization of 2 without losing activity against the HCV protease, the proton at that chiral site was replaced with deuterium (d). The compound 1 (d-telaprevir) is as efficacious as 2 in in vitro inhibition of protease activity and viral replication (replicon) assays. The kinetics of in vitro stability of 1 and 2 in buffered pH solutions and plasma samples, including human plasma, suggest that 1 is significantly more stable than 2. Oral administration (10 mg/kg) in rats resulted in a approximately 13% increase of AUC for 1. | lld:pubmed |
| pubmed-article:19894743 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19894743 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19894743 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19894743 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:19894743 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:PazhanisamySS | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:MittletonM... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:HoweDavidD | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:BennaniYousse... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:MaltaisFranço... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:LaitinenLeena... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:MaChienC | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:HuangHuiH | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:ManiNagrajN | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:JungYoung... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:PerniRobert... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:BlockEricE | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:NamchukMarkM | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:GaoHongyingH | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:RaybuckScottS | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:TownChristoph... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:BrummelChrist... | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:ChenMinzhangM | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:TanouryJerryJ | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:LiaoShengkaiS | lld:pubmed |
| pubmed-article:19894743 | pubmed:author | pubmed-author:TsaoHongH | lld:pubmed |
| pubmed-article:19894743 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19894743 | pubmed:day | 24 | lld:pubmed |
| pubmed-article:19894743 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:19894743 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19894743 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19894743 | pubmed:pagination | 7993-8001 | lld:pubmed |
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| pubmed-article:19894743 | pubmed:meshHeading | pubmed-meshheading:19894743... | lld:pubmed |
| pubmed-article:19894743 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19894743 | pubmed:articleTitle | In vitro and in vivo isotope effects with hepatitis C protease inhibitors: enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats. | lld:pubmed |
| pubmed-article:19894743 | pubmed:affiliation | Vertex Pharmaceuticals Incorporated, Cambridge, Massachusetts 02139, USA. | lld:pubmed |
| pubmed-article:19894743 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:19894743 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19894743 | lld:chembl |
