Orally active, potent and selective HIV type-1 (HIV-1) integrase inhibitor in cultures and in vivo.
Raltegravir (MK-0518) is an orally active, potent and selective HIV type-1 (HIV-1) integrase inhibitor (IC50 = 2-7 nM; ineffctive against HIV-1 reverse transcriptase or protease) that prevents HIV-1 cellular replication by blocking viral cDNA integration into host genome in cultures (IC50 = 19 nM & 33 nM in the presence of 10% fetal bovine serum or 50% human serum) and in vivo.
* Raltegravir, the first in a new class of orally administered HIV type-1 (HIV-1) integrase inhibitors, selectively inhibits the strand transfer activity of HIV-1 and its integration into human DNA, a key stage in retroviral propagation, thereby limiting viral replication
To assess the potential direct effects of the integrase strand-transfer inhibitors (INsTIs) dolutegravir, bictegravir, and raltegravir, drugs used as treatment for people living with human immunodeficiency virus (PLWH), on human adipose cells. Drugs were added to the differentiation medium of
Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals
Journal of Acquired Immune Deficiency Syndromes, 43(5), 509-515 (2006)
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