Center for the AIDS Program of Research in South Africa (CAPRISA), Nelson R Mandela School of Medicine, University of KwaZulu Natal, Durban, South Africa.
Discipline of Pharmacology, College of Health Sciences, University of KwaZulu-Natal, Durban, South Africa.
Expert Rev Clin Pharmacol. 2023 Jul-Dec;16(10):939-957. doi: 10.1080/17512433.2023.2251387. Epub 2023 Sep 7.
Tenofovir alafenamide (TAF), a prodrug of tenofovir, achieves higher intracellular concentrations of tenofovir-diphosphate and 90% lower plasma concentrations of tenofovir compared to tenofovir disoproxil fumarate (TDF). TAF is associated with improved renal and bone safety outcomes.
We review the efficacy and safety of TAF-containing regimens in adults and pediatrics. We highlight safety data during pregnancy, drug interactions during co-administration with tuberculosis treatment, and critical knowledge gaps to be addressed for the successful implementation of TAF in low- and middle-income countries. We performed a search on MEDLINE PubMed and conference websites for relevant articles published from January 2010 to March 2023.
Current evidence demonstrates that TAF has similar efficacy and tolerability, superior bone and renal safety, and higher rates of dyslipidemia and weight gain, compared with TDF. However, there are several knowledge gaps, in specific sub-populations, that require action. Emerging data suggests that TAF is safe during pregnancy, although fuller safety data to support TAF use in pregnancy is needed. Similarly, there is a lack of evidence that TAF can be used in combination with rifamycin-based tuberculosis treatment in PWH and TB. Further studies are needed to fill knowledge gaps and support the wider rollout of TAF.
替诺福韦艾拉酚胺（TAF）是替诺福韦的前药，与富马酸替诺福韦二吡呋酯（TDF）相比，它能使替诺福韦二磷酸酯在细胞内的浓度更高，而替诺福韦在血浆中的浓度降低 90%。TAF 与改善肾脏和骨骼安全性结局相关。
我们综述了含 TAF 方案在成人和儿科患者中的疗效和安全性。我们强调了妊娠期间的安全性数据、与结核病治疗联合用药时的药物相互作用，以及为在中低收入国家成功实施 TAF 而需要解决的关键知识空白。我们在 MEDLINE PubMed 和会议网站上搜索了 2010 年 1 月至 2023 年 3 月期间发表的相关文章。
目前的证据表明，与 TDF 相比，TAF 具有相似的疗效和耐受性，在骨骼和肾脏安全性方面更优，且血脂异常和体重增加的发生率更高。然而，在特定亚人群中，仍存在一些需要采取行动的知识空白。新出现的数据表明，TAF 在妊娠期间是安全的，尽管需要更多的安全性数据来支持 TAF 在妊娠期间的使用。同样，也缺乏证据表明 TAF 可与利福平为基础的结核病治疗联合用于 HIV 感染者和结核病患者。需要进一步研究来填补知识空白并支持 TAF 的更广泛应用。
