Simplified model of PK of remdesivir
Remdesivir (RDV) GS-5734 is antiviral to treat COVID-19, it is a
prodrug of an adenosine analogue.
As Remdesivir bioavailability is almost 0 it is not fit for
oral administration, thus intravenous administration is recommended
first dose 200mg and other 4 - 10 doses per 100 mg every 24 h with
intravenous application typically 30-60 minutes.
RDV is taken by target cell and metabolized in multiple steps
(utilizing enzymes hydrolaze, phosphataze) to form active form
GS-443902. It is also metabolised (nucleotidase) to nonactive form
GS-441524.
Critical is concentration of active form in target
cells.
RDV, active and non_active have different clearance rate
elimination by kidneys/liver.
[1] Li, R., Liclican, A., Xu, Y., Pitts, J., Niu, C., Zhang,
J., Kim, C., Zhao, X., Soohoo, D., Babusis, D., Yue, Q., Ma, B.,
Murray, B. P., Subramanian, R., Xie, X., Zou, J., Bilello, J. P.,
Li, L., Schultz, B. E., … Feng, J. Y. (2021). Key metabolic enzymes
involved in Remdesivir activation in human lung cells.
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https://doi.org/10.1128/AAC.00602-21
[2] Humeniuk, R., Mathias, A., Cao, H., Osinusi, A., Shen, G.,
Chng, E., Ling, J., Vu, A., & German, P. (2020). Safety,
Tolerability, and Pharmacokinetics of Remdesivir, An Antiviral for
Treatment of COVID-19, in Healthy Subjects. Clinical and
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https://doi.org/10.1111/cts.12840
2025 Tomas Kulhanek, Ph.D., VITO NV
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