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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

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rdf:type
rdfs:label
  • MK-2048 (fr)
  • MK-2048 (en)
  • MK-2048 (zh)
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. (fr)
  • 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。 (zh)
  • 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 (en)
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  • http://commons.wikimedia.org/wiki/Special:FilePath/MK-2048.svg
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  • none (en)
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  • MK-2048 (en)
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legal US
  • Investigational New Drug (en)
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PubChem
SMILES
  • CCN1CCC (en)
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StdInChIKey
  • IOYLKNABOQYKKY-JTQLQIEISA-N (en)
UNII
  • LJ8U884TM5 (en)
has 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". (en)
  • 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. (fr)
  • 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。 (zh)
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page length (characters) of wiki page
CAS number
  • 869901-69-9
ChEMBL
  • 1237018
FDA UNII code
  • LJ8U884TM5
PubChem
  • 11554427
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