Peramivir trihydrate (RWJ-270201, BCX-1812) is a highly potent, selective and orally active influenza virus neuraminidase (NA) inhibitor, with IC50 values ranging from 0.9 to 4.3 nM for nine NA subtypes. RWJ-270201 has efficacy comparable to or better than earlier NA inhibitors against a wide range of influenza A and B isolates, including recently emerged and avian strains, both in vitro and in a lethal murine model of influenza[3]. Peramivir is effective against a variety of influenza A and B subtypes and has a lower half-maximal inhibitory concentration compared to other NAIs in in vitro studies. The long half-life of peramivir allows for once-daily dosing. The drug is eliminated primarily by the kidneys, warranting dose adjustments in patients with renal dysfunction[4]. Peramivir is administered as a single-dose via the intravenous route providing a valuable therapeutic alternative for critically ill patients or those unable to tolerate other administration routes[5].
Peramivir Trihydrate/帕拉米韦 三水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MDCK-hPEPT1 cells
0.5 mM
10 min
Evaluate the uptake of Peramivir-(CH2)2-l-Val and Peramivir-l-Ile in MDCK-hPEPT1 cells, results showed that the uptake of these two prodrugs was significantly higher than in mock cells and could be inhibited by gly-sar, indicating their uptake is mediated by PEPT1.
Asian J Pharm Sci. 2018 Nov;13(6):555-565.
Caco-2 cells
0.5 mM
120 min
Evaluate the permeability of Peramivir and its prodrugs in Caco-2 cells, results showed that all prodrugs had higher permeability than Peramivir, with Peramivir-(CH2)2-l-Val and Peramivir-l-Ile showing the highest permeability.
Asian J Pharm Sci. 2018 Nov;13(6):555-565.
Human Peripheral Blood Mononuclear Cells (hPBMCs)
2.5, 5, 10 μM
6 or 12 h
To evaluate the inhibitory effect of Peramivir on TNF-α, results showed that Peramivir significantly inhibited TNF-α release at 6 h and 12 h in a time- and dose-dependent manner.
Front Immunol. 2022 Feb 28;13:856327.
Macrophages
10 µM
4 h
To evaluate the inhibitory effect of Peramivir on TNF-α, results showed that Peramivir inhibited TNF-α release by 67.2% at 10 µM.
Front Immunol. 2022 Feb 28;13:856327.
Peramivir Trihydrate/帕拉米韦 三水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
LPS-induced cytokine storm model
Intraperitoneal injection
20 mg/kg, 60 mg/kg
Single injection
To evaluate the inhibitory effect of Peramivir on cytokine storm, results showed that Peramivir significantly reduced multiple cytokines in serum and bronchoalveolar lavage fluid (BALF), alleviated acute lung injury, and prolonged the survival time of mice.
搜索
