Department of Microbiology, Immunology & Transplantation, Rega Institute for Medical Research, KU Leuven, Belgium.
Antivir Chem Chemother. 2023 Jan-Dec;31:20402066231152971. doi: 10.1177/20402066231152971.
Brivudin, (()-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) can be considered the gold standard for the treatment of varicella-zoster virus (VZV) infections, such as herpes zoster (shingles). It is available for clinical use in most European countries (except for the UK) and over the whole world (except for the US and Canada). Besides VZV its activity spectrum also includes various other herpesviruses, such as herpes simplex virus type 1 (HSV-1). Its activity against VZV and HSV-1 depends on phosphorylation by the virus-encoded thymidine kinase (TK). In its active form (BVDU TP or BVDU 5'-triphosphate), it can act as both substrate and inhibitor of the viral (i.e., HSV-1) DNA polymerase. It has proven to be effective against herpes zoster, including post-herpetic neuralgia (PHN). It is contra-indicated in patients concomitantly treated by 5-fluorouracil (FU), since its degradation product, ()-5-(2-bromovinyl)uracil, is inhibitory to the catabolism of FU, which may enhance the toxicity of the latter. A new compound, the bicyclic nucleoside analogue (BCNA) Cf-1743, has been described, which is a more potent inhibitor of VZV replication than BVDU and which does not interfere with the catabolism of FU. It is applicable orally, as its 5'-valine ester FV-100 (Fermavir), but has not (yet) been marketed for clinical use.
溴夫定（()-5-(2-溴乙烯基)-2'-脱氧尿苷（BVDU）可被视为治疗水痘带状疱疹病毒（VZV）感染的金标准，如带状疱疹（带状疱疹）。它在大多数欧洲国家（英国除外）和全世界（美国和加拿大除外）都可用于临床。除了 VZV，它的活性谱还包括其他各种疱疹病毒，如单纯疱疹病毒 1 型（HSV-1）。它对 VZV 和 HSV-1 的活性取决于病毒编码的胸苷激酶（TK）的磷酸化。在其活性形式（BVDU TP 或 BVDU 5'-三磷酸）中，它可以作为病毒（即 HSV-1）DNA 聚合酶的底物和抑制剂。它已被证明对带状疱疹有效，包括带状疱疹后神经痛（PHN）。它在同时接受氟尿嘧啶（FU）治疗的患者中被禁忌，因为其降解产物（)-5-(2-溴乙烯基)尿嘧啶对 FU 的分解代谢具有抑制作用，这可能会增强后者的毒性。一种新的化合物，双环核苷类似物（BCNA）Cf-1743，已被描述，它是一种比 BVDU 更有效的 VZV 复制抑制剂，并且不干扰 FU 的分解代谢。它可口服应用，因为其 5'-缬氨酸酯 FV-100（Fermavir），但尚未（尚未）用于临床。
