Oseltamivir is an inhibitor of influenza neuraminidase, with IC₅₀ values of 13nM, 1.34nM, 0.9nM, and 0.67nM against Influenza B, A/H1N1, A/H1N2, and A/H3N2 viruses, respectively[1]. As a neuraminidase inhibitor, Oseltamivir attenuates the penetration of viruses through the mucus on the respiratory tract and inhibits the release of virus progeny from infected cells[2].
In vitro, with 3 days of treatment, Oseltamivir at 0.0125nM showed partial inhibition, whereas concentrations above 0.05nM showed complete inhibition in H1N1 IVA-infected MDCK cells[2]. Oseltamivir (500-800μg/mL; 24-72h) inhibited the viability of MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner[3].
In vivo, in BALB/c mice infected with the H3N1 influenza virus, Oseltamivir (1 and 10mg/kg/d; p.o.; twice daily from 4 hours before infection to 5 days post-infection) dose-dependently reduced total cells, neutrophils, macrophages, and pro-inflammatory cytokines in bronchoalveolar lavage fluid (BALF)[4].
References:
[1] Ferraris, O et al. “Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice.” Antiviral research vol. 68,1 (2005): 43-8.
[2] Chan RWY, Tao KP, Ye J, et al. Inhibition of Influenza Virus Replication by Oseltamivir Derivatives. Pathogens. 2022;11(2):237.
[3] Haxho F, Allison S, Alghamdi F, et al. Oseltamivir phosphate monotherapy ablates tumor neovascularization, growth, and metastasis in mouse model of human triple-negative breast adenocarcinoma. Breast Cancer (Dove Med Press). 2014;6:191-203.
[4] Wong ZX, Jones JE, Anderson GP, Gualano RC. Oseltamivir treatment of mice before or after mild influenza infection reduced cellular and cytokine inflammation in the lung. Influenza Other Respir Viruses. 2011;5(5):343-350.
Oseltamivir是一种流感神经氨酸酶抑制剂，对Influenza B，A/H1N1，A/H1N2和A/H3N2 病毒的IC₅₀值分别为13nM，1.34nM，0.9nM和0.67nM[1]。作为一种神经氨酸酶抑制剂，Oseltamivir可以减弱病毒通过呼吸道粘液的渗透，并抑制病毒子代从感染细胞释放[2]。
体外实验中，经3天处理，Oseltamivir在0.0125nM时对H1N1 IVA感染的MDCK细胞表现为部分抑制，而在高于0.05nM的浓度下表现为完全抑制[2]。Oseltamivir（500-800μg/mL；24-72h）以剂量依赖和时间依赖的方式抑制MDA-MB-231和MCF-7细胞的活力[3]。
体内实验中，在感染H3N1流感病毒的BALB/c小鼠中，Oseltamivir（1和10mg/kg/天；灌胃；自感染前4小时至感染后5天，每日2次）以剂量依赖方式降低支气管肺泡灌洗液（BALF）中的总细胞数、中性粒细胞、巨噬细胞及促炎性细胞因子水平[4]。