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TENOFOVIR ALAFENAMIDE FUMARATE FOR THE TREATMENT OF HIV INFECTION

机译:Tenofovir Alafenamide富马酸莫特治疗艾滋病毒感染

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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:Tenofovir Alafenamide富马酸莫酸盐是替诺福韦的最近开发的前药,一种核苷酸类似物逆转录酶抑制剂,具有抗HIV的有效抑制活性。 先前开发的替诺福韦前药,替诺福韦毒性富马酸核的效用受到肾病和骨矿物不良事件的阻碍。 Tenofovir Alafenamide富马特通过提供高细胞内浓度的父毒药物Tenofovir而克服了替诺福韦毒素富马酸骨的缺点,同时大大减少了全身暴露。 Tenofovir Alafenamide富马酸莫汀目前可作为三种固定剂量产品的组分提供:I)与Emtrickingabine的Coformulation; ii)用ElviteGravir,Cobicistat和Emtrickabine的Coformulation; 和III)与瑞培和梅特菌的共焦。

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