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Statements

Subject Item
dbr:MK-2048
rdf:type
yago:Matter100020827 yago:WikicatIntegraseInhibitors owl:Thing yago:Agent114778436 yago:CausalAgent100007347 yago:Drug103247620 wikidata:Q8386 n20:ChemicalObject yago:Substance100020090 dbo:Drug dbo:ChemicalSubstance yago:Inhibitor114724436 yago:PhysicalEntity100001930
rdfs:label
MK-2048 MK-2048 MK-2048
rdfs:comment
MK-2048 est une molécule de la classe des anti-intégrase, développée par Merck & Co. Elle est actuellement[Quand ?] en essais cliniques de phase II. La molécule offre un différent de ceux du raltégravir et de l'elvitégravir, et les personnes ayant développé des résistances à ces médicaments pourront donc bénéficier du MK-2048, décrit comme inhibiteur d'intégrase de nouvelle génération. MK-2048 is the Merck & Co. designation for a molecule in its pre-clinical drug discovery that is an integrase inhibitor-class of agent intended to be used against HIV infection. It is a second generation integrase design thought to be superior to the first available integrase inhibitor, raltegravir, in that "MK-2048 has a dissociation half-life of 32 hours on wild-type integrase—more than four times that of raltegravir", and its dissociation half-life against the important HIV integrase mutant N155H was on the same order of magnitude as that of raltegravir against wild-type virus, leading the Merck presenter to suggest the possibility of "reduced susceptibility to resistance mutations" for the second generation drug. MK-2048 is being investigated for use as part of a pre-exposure prophylax MK-2048系第二代整合酶抑制剂，是抗病毒药品，用于对抗HIV感染。其较前代整合酶抑制剂药物拉替拉韦的优点是，该药物对HIV整合酶的有效抑制时间长达4倍。MK-2048作为暴露前阻断药物（PrEP）的实用性正在研究当中。 MK-2048由默克藥廠开发。
foaf:depiction
n11:MK-2048.svg
dcterms:subject
dbc:Experimental_drugs dbc:Integrase_inhibitors
dbo:wikiPageID
25019159
dbo:wikiPageRevisionID
1123276051
dbo:wikiPageWikiLink
dbr:Discovery_and_development_of_integrase_inhibitors dbr:Pre-exposure_prophylaxis dbc:Experimental_drugs dbr:Merck_&_Co. dbr:HIV dbr:Raltegravir dbc:Integrase_inhibitors
owl:sameAs
dbpedia-sh:MK-2048 yago-res:MK-2048 dbpedia-fr:MK-2048 wikidata:Q3273019 dbpedia-zh:MK-2048 freebase:m.09gmb7p n23:32CCU dbpedia-sr:MK-2048 dbpedia-vi:MK-2048
dbp:wikiPageUsesTemplate
dbt:Full dbt:Third_party dbt:Update dbt:Cascite dbt:Antiinfective-drug-stub dbt:Reflist dbt:Multiple_issues dbt:Fdacite dbt:Infobox_drug dbt:Antiretroviral_drug
dbo:thumbnail
n11:MK-2048.svg?width=300
dbp:atcPrefix
none
dbp:c
21
dbp:caption
MK-2048
dbp:casNumber
869901
dbp:chembl
1237018
dbp:chemspiderid
25058456
dbp:cl
1
dbp:f
1
dbp:h
21
dbp:iupacName
-2
dbp:legalUs
Investigational New Drug
dbp:n
5
dbp:o
4
dbp:pubchem
11554427
dbp:smiles
CCN1CCC
dbp:stdinchi
1
dbp:stdinchikey
IOYLKNABOQYKKY-JTQLQIEISA-N
dbp:unii
LJ8U884TM5
dbo:abstract
MK-2048 is the Merck & Co. designation for a molecule in its pre-clinical drug discovery that is an integrase inhibitor-class of agent intended to be used against HIV infection. It is a second generation integrase design thought to be superior to the first available integrase inhibitor, raltegravir, in that "MK-2048 has a dissociation half-life of 32 hours on wild-type integrase—more than four times that of raltegravir", and its dissociation half-life against the important HIV integrase mutant N155H was on the same order of magnitude as that of raltegravir against wild-type virus, leading the Merck presenter to suggest the possibility of "reduced susceptibility to resistance mutations" for the second generation drug. MK-2048 is being investigated for use as part of a pre-exposure prophylaxis (PrEP) approach to the treatment of HIV infection. At the time of these reports, there was no indication of the time by which "MK-2048, or related compounds, [would] be ready for clinical trials". MK-2048 est une molécule de la classe des anti-intégrase, développée par Merck & Co. Elle est actuellement[Quand ?] en essais cliniques de phase II. La molécule offre un différent de ceux du raltégravir et de l'elvitégravir, et les personnes ayant développé des résistances à ces médicaments pourront donc bénéficier du MK-2048, décrit comme inhibiteur d'intégrase de nouvelle génération. MK-2048系第二代整合酶抑制剂，是抗病毒药品，用于对抗HIV感染。其较前代整合酶抑制剂药物拉替拉韦的优点是，该药物对HIV整合酶的有效抑制时间长达4倍。MK-2048作为暴露前阻断药物（PrEP）的实用性正在研究当中。 MK-2048由默克藥廠开发。
gold:hypernym
dbr:Inhibitor
prov:wasDerivedFrom
wikipedia-en:MK-2048?oldid=1123276051&ns=0
dbo:wikiPageLength
4176
dbo:casNumber
869901-69-9
dbo:chEMBL
1237018
dbo:fdaUniiCode
LJ8U884TM5
dbo:pubchem
11554427
foaf:isPrimaryTopicOf
wikipedia-en:MK-2048