| Description | Netivudine is a potent nucleoside reverse transcriptase inhibitor (NRTIs), a nucleoside analogue with anti-varicella zoster virus activity that can be used to treat human immunodeficiency virus (HIV) infection. Netivudine works by inhibiting reverse transcriptase, which reduces viral load in the body and slows the progression of the disease through its inhibitory effect. |
| In vitro | 在人类细胞中，受VZV感染后，netivudine的磷酸化作用与sorivudine相似，其对VZV的IC50值介于0.6-3.8 uM之间。在HSV感染的细胞中，netivudine仅形成单磷酸盐，因此对HSV或其他人类疱疹病毒没有明显的体外活性。[1] |
| In vivo | Netivudine在人体中的半衰期约为12-15小时。通过对年轻成年人和健康的老年志愿者采用100 mg、200 mg及400 mg口服剂量的初步药代动力学研究确认，每日两次给药可以达到并维持远高于VZV IC50的化合物浓度。[2]在年轻人和老年人中，化合物的生物利用度分别为21.1%和24.6%。一项初步的、开放的、剂量范围研究，针对31名患有局部带状疱疹的老年免疫力正常患者，通过每日两次最高200mg的口服剂量，展示了Netivudine在疹子愈合和疼痛治疗上的疗效，且没有显著的不良反应。[3] |
| Target activity | VZV:0.6-3.8μM |
| molecular weight | 282.25 |
| Molecular formula | C12H14N2O6 |
| CAS | 84558-93-0 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (194.86 mM) |
| References | 1. Rahim S G, et al. 5-Alkynyl pyrimidine nucleosides as potent selective inhibitors of varicella-zoster virus. Antiviral Chemistry and Chemotherapy. 1992;3(5): 293-297. 2. Peck RW, et al. The bioavailability and disposition of 1-(beta-D-arabinofuranosyl)-5-(1-propynyl)uracil (882C87), a potent, new anti-varicella zoster virus agent. Br J Clin Pharmacol. 1995;39(2):143-149. 3. Wood MJ, et al. Preliminary pharmacokinetics and safety of 882C87 in patients with herpes zoster. J Med Virol. 1993;1:154-157. |