Abstract
Remdesivir is one of the most encouraging treatments against SARS-CoV-2 infection. After intravenous infusion, RDV is rapidly metabolized (t 1/2 = 1 h) within the cells to its active adenosine triphosphate analogue form (GS-443902) and then it can be found in plasma in its nucleoside analogue form (GS-441524). In this real-life study, we describe the remdesivir and GS-441524 concentrations at three time points in nine ICU patients, through a validated ultra-high-performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) method. The observed data confirmed the very rapid conversion of RDV to its metabolite and the quite long half-life of GS-441524. The mean C min , C max and AUC 0-24 , were < 0.24 ng/mL and 122.3 ng/mL, 2637.3 ng/mL and 157.8 ng/mL, and 5171.2 ng*h/mL and 3676.5 ng*h/ml, respectively, for RDV and GS-441524. Three out of nine patients achieved a C max > 2610 ng/mL and 140 ng/mL and AUC 0-24 > 1560 ng*h/mL and 2230 ng*h/mL for RDV and GS-441524, respectively. The mean t 1/2 value for GS-441524 was 26.3 h. Despite the low number of patients, these data can represent an interesting preliminary report on the variability of RDV and GS-441524 concentrations in a real-life ICU setting.
Keywords: COVID-19; ICU; SARS-CoV-2; pharmacokinetics; pneumonia; remdesivir.
【저자키워드】 COVID-19, SARS-CoV-2, Pneumonia, pharmacokinetics, ICU, remdesivir., 【초록키워드】 Treatment, mass spectrometry, SARS-COV-2 infection, Remdesivir, triphosphate, pharmacokinetics, Liquid chromatography, Patient, GS-441524, plasma, ICU Patients, patients, adenosine, metabolite, RDV, Tandem mass spectrometry, Concentration, AUC, intravenous, intravenous infusion, adenosine triphosphate, These data, Variability, nucleoside, C max, preliminary report, UHPLC, Cell, nine, 【제목키워드】 Severe COVID-19 pneumonia, Pneumonia, pharmacokinetic, ICU patient,