Department of Pharmacy, NYU Langone Hospital, Brooklyn, NY, USA.
College of Pharmacy and Health Sciences, St. John's University, Queens, NY, USA.
J Int Assoc Provid AIDS Care. 2020 Jan-Dec;19:2325958220919231. doi: 10.1177/2325958220919231.
HIV is a serious chronic medical condition. Significant improvements in antiretroviral therapy have led to a transformation in its management. No curative treatment is available for HIV, and lifelong therapy is required with a combination of agents to control viral replication and prevent complications. Some of the older agents are notorious for many side effects, making patient compliance difficult, which is critical to preventing HIV resistance. Tenofovir is one of the newer, more tolerable, nucleotide reverse transcriptase inhibitors on the market; is a mainstay of many antiretroviral therapy combinations; and is now available in 2 different formulations, tenofovir disoproxil fumarate (TDF) and, the more recent, tenofovir alafenamide (TAF). These 2 formulations have very different pharmacokinetics, which seem to affect their efficacy and safety. This manuscript provides insight into the history of TDF and TAF development, their unique pharmacokinetics and pharmacology, clinically important adverse effects, monitoring, interactions, resistance, review of clinical studies, and guideline recommendations and clinical applications for tenofovir's various indications.
HIV 是一种严重的慢性疾病。抗逆转录病毒疗法的显著进步使得其治疗方式发生了转变。目前尚无治愈 HIV 的方法，需要终身联合使用多种药物来控制病毒复制并预防并发症。一些较老的药物因副作用多而臭名昭著，这使得患者难以坚持治疗，而坚持治疗对于预防 HIV 耐药至关重要。替诺福韦是市场上较新的、耐受性更好的核苷酸逆转录酶抑制剂之一；是许多抗逆转录病毒治疗组合的基础；现在有两种不同的制剂，富马酸替诺福韦二吡呋酯（TDF）和最近的替诺福韦艾拉酚胺（TAF）。这两种制剂具有非常不同的药代动力学特性，这似乎影响了它们的疗效和安全性。本文介绍了 TDF 和 TAF 的开发历史、它们独特的药代动力学和药理学、临床上重要的不良反应、监测、相互作用、耐药性、临床研究综述以及替诺福韦各种适应证的指南建议和临床应用。
