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. 2021 Dec 30:eabl828. doi: 10.1126/scitranslmed.abl8282

Table 1. Systemic pharmacokinetic parameters of remdesivir (RDV) and key metabolites were measured after intravenous (IV) and inhalation routes of administration.

Plasma concentrations of RDV and its alanine metabolite and nucleoside metabolite were measured after a single dose of RDV administered to AGM by IV (10 mg/kg; n=3) or inhalation (5 mg/mL for 30 or 90 min resulting in deposited doses of 0.17 and 0.54 mg/kg, respectively, n=4 per dose) routes. Cmax and AUClast values presented are the mean ± SD for each analyte and treatment group. Data for each analyte were analyzed using a one-way ANOVA with Dunnett post-hoc correction, and presented p values represent comparison of each inhalation dose group with the IV dose group.

Analyte RDV Route, Dose Plasma PK Parameter
Cmax (μM) p Value AUClast (μM•hr) p Value
Remdesivir IV, 10 mg/kg 12.6 ± 1.0 N/A 7.26 ± 1.29 N/A
Inhalation, 0.17 mg/kg 0.04 ± 0.01 <0.0001 0.02 ± 0.01 <0.0001
Inhalation, 0.54 mg/kg 0.10 ± 0.02 <0.0001 0.15 ± 0.05 <0.0001
Alanine metabolite IV, 10 mg/kg 15.9 ± 4.9 N/A 9.47 ± 1.07 N/A
Inhalation, 0.17 mg/kg 0.16 ± 0.06 <0.0001 0.13 ± 0.03 <0.0001
Inhalation, 0.54 mg/kg 0.23 ± 0.03 <0.0001 0.42 ± 0.05 <0.0001
Nucleoside metabolite IV, 10 mg/kg 1.23 ± 0.36 N/A 9.06 ± 2.60 N/A
Inhalation, 0.17 mg/kg 0.03 ± 0.01 <0.0001 0.19 ± 0.03 <0.0001
Inhalation, 0.54 mg/kg 0.07 ± 0.01 <0.0001 0.54 ± 0.08 <0.0001