Raltegravir monohydrate
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چکیده
منابع مشابه
Raltegravir monohydrate
THE HYDRATED TITLE COMPOUND [SYSTEMATIC NAME: N-(4-fluoro-benz-yl)-5-hy-droxy-1-methyl-2-{1-methyl-1-[(5-methyl-1,3,4-oxa-diazol-2-ylcarbon-yl)amino]-eth-yl}-6-oxo-1,6-di-hydro-pyrimidine-4-carb-oxamide monohydrate], C20H21FN6O5·H2O, is recognised as the first HIV integrase inhibitor. In the mol-ecule, the dihedral angles between the mean planes of the pyrimidine ring and the phenyl and oxa-dia...
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Similar to all antiretroviral drugs, failure of raltegravir-based treatment regimens to fully supress HIV replication almost invariably results in emergence of HIV resistance to this new drug. HIV resistance to raltegravir is the consequence of mutations located close to the integrase active site, which can be divided into three main evolutionary pathways: the N155H, the Q148R/H/K and the Y143R...
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Raltegravir is the first integrase inhibitor approved for the treatment of HIV infection based on the superior efficacy it showed compared to optimized backbone therapy alone in patients harboring multidrug resistant viruses. Studies on naive patients showed comparable efficacy of raltegravir and efavirenz and just recently the US Food and Drug Administration (FDA) approved raltegravir for the ...
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Raltegravir (Isentress) is the first approved HIV integrase inhibitor. Agents in this class target a different viral enzyme compared with agents inhibiting reverse transcriptase and protease. A wide number of patients are currently susceptible to integrase inhibitors, including heavily antiretroviral-experienced patients harbouring drug-resistant viruses. The good tolerability and convenience o...
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Raltegravir, the first approved integrase inhibitor, has been shown to be virologically effective in Phase II and Phase III clinical trials in both treatment naive and triple class resistant patients. It also has an excellent tolerability profile and lacks significant drug-drug interactions making it an important drug in the treatment of a number of special patient populations. In this review i...
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ژورنال
عنوان ژورنال: Acta Crystallographica Section E Structure Reports Online
سال: 2013
ISSN: 1600-5368
DOI: 10.1107/s1600536813029747