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TENOFOVIR ALAFENAMIDE FUMARATE FOR THE TREATMENT OF HIV INFECTION

机译:富马酸替诺福尔阿芬酰胺治疗艾滋病毒感染

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摘要

Tenofovir alafenamide fumarate is a recently developed prodrug of tenofovir, a nucleotide analogue reverse transcriptase inhibitor with potent inhibitory activity against HIV. The utility of a previously developed tenofovir prodrug, tenofovir disoproxil fumarate, had been hampered by renal and bone mineral adverse events. Tenofovir alafenamide fumarate overcomes the shortcomings of tenofovir disoproxil fumarate by delivering high intracellular concentrations of the parent drug, tenofovir, while substantially reducing systemic exposure. Tenofovir alafenamide fumarate is currently available as a component of three fixed-dose products: i) coformulation with emtricitabine; ii) coformulation with elvitegravir, cobicistat and emtricitabine; and iii) coformulation with rilpivirine and emtricitabine.
机译:替诺福韦阿拉芬酰胺富马酸酯是替诺福韦的最新开发产品,替诺福韦是一种核苷酸类似物逆转录酶抑制剂,对HIV具有强抑制活性。先前开发的替诺福韦前药(富马酸替诺福韦二甲氧苄啶)的实用性受到肾脏和骨骼矿物质不良事件的阻碍。替诺福韦阿拉芬酰胺富马酸酯通过提供高浓度的母体药物替诺福韦细胞内浓度,同时大大降低了全身暴露,克服了替诺福韦双酚福马酸酯的缺点。替诺福韦阿拉芬酰胺富马酸酯目前可作为三种固定剂量产品的成分使用:i)与恩曲他滨共同配制; ii)与elvitegravir,cobicistat和恩曲他滨共同配制; iii)与利比韦林和恩曲他滨共同配制。

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