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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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  • 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 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。
  • 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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  • none
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  • MK-2048
CAS number
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legal US
  • Investigational New Drug
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  • CCN1CCC
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  • IOYLKNABOQYKKY-JTQLQIEISA-N
UNII
  • LJ8U884TM5
has abstract
  • MK-2048 est une molécule de la classe des anti-intégrase, développée par Merck & Co. Elle est actuellement 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 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。
CAS number
  • 869901-69-9
ChEMBL
  • 1237018
FDA UNII code
  • LJ8U884TM5
PubChem
  • 11554427
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