San Francisco, CA, USA.
Akero Therapeutics, South San Francisco, CA, USA.
Antivir Ther. 2022 Apr;27(2):13596535211067600. doi: 10.1177/13596535211067600.
Tenofovir alafenamide fumarate is a lipophilic prodrug of tenofovir which is preferentially metabolized in lymphatic tissue resulting in high concentrations of tenofovir (TFV) and its active diphosphate metabolite inside the cells that replicate HIV. Due to its selectivity for these tissues, lower total doses of TAF can be administered relative to tenofovir disoproxil fumarate (TDF) which results in improved bone and renal biomarkers. Tenofovir alafenamide fumarate has become the "backbone" of multiple combination products for the treatment of HIV, combined with emtricitabine for PreP and as a monotherapy for the treatment or HBV.
富马酸替诺福韦艾拉酚胺是替诺福韦的一种脂溶性前药，在淋巴组织中优先代谢，导致细胞内替诺福韦（TFV）及其活性二磷酸代谢物浓度升高，从而复制 HIV。由于其对这些组织的选择性，相对于富马酸替诺福韦二吡呋酯（TDF），可以给予较低的总替诺福韦艾拉酚胺剂量，从而改善骨和肾脏生物标志物。富马酸替诺福韦艾拉酚胺已成为多种用于治疗 HIV 的联合产品的“骨干”，与恩曲他滨联合用于 PrEP，也可作为治疗或 HBV 的单一疗法。
