Ivermectin as a potential COVID-19 treatment from the pharmacokinetic point of view

Georgi Momekov; Denitsa Momekova

The copyright holder for this preprint (which was not peer-reviewed) is the . https://doi.org/10.1101/2020.04.11.20061804 doi: medRxiv preprint Table 2 . Comparison between the in vitro inhibitory concentration of ivermectin 11 with exemplar published C max values of the drug 12, 17 In vitro end-points 11 Inhibitory concentrations (µmol/L) The repurposed antimalarial drugs hydroxychloroquine and chloroquine that have been included in numerous COVID-19 treatment protocols also have micromolar inhibitory concentrations against SARS-CoV-2 26 and nanomolar C max values 27 . Nevertheless these agents have enormous apparent volumes of distribution and presumably disproportionally larger tissue levels relative to the plasma concentrations, which makes the translation of the in vitro data plausible [27] [28] [29] . The other very promising agent tested in clinical trials and applied as compassionate use for COVID-19 is remdesivir 1,30 . This broad-spectrum antiviral drug originally developed for Ebola shows potent inhibitory effects against SARS-CoV-2 with an IC 50 of 0.77 µmol/L (464 ng/ml) 31 . This concentration is readily attainable as the drug is given as venous infusion. The typical dosing schedule for remdesivirinitial infusion of 200 mg, followed by 100 mg/daily for a total of 5 days yields maximal plasma concentrations of 5440 ng/ml in the first day and 2610 on day 5 30 .