Unfortunately, most data are missed for antiviral e.g Remidisvir
i want to speculate plasma/ lung ?? or any alternative measure
We estimated Vd of this antiviral drug from published data dose. in human
dose 100 mg IV I,e 100 X 1000X 1000 ng Cmx = about 2000 ng/ ml ( I have the exact calculations ) Vd = dose/ Cmax = 50 000 ml = 50 L for 70 kg about 0.6-0.7 L/kg However, what is the clinical impact ?? . The drug is metabolized within the cell to the active metabolite, ( entrapped ) this is a positive point but the half-life of active metabolite 16 hr. within the cell How we can speculate the efficacy of viral pneumonia. Is this drug access lung tissue inadequate level, which explains low efficacy with the current regimen ?? The drug is very active in Vitro, IC50 = 0.7 u mol C min of active metabolite NTP = 7 micromol/ ml ( NTP = nucleotide analog triphosphate ) It is a very difficult task, I am not sure ?? try to ask other experts. If he came to the same conclusion Currently, my hypothesis this drug will not show high efficacy. in case of high viral load ( severe cases ) . will not save the life It may act in moderate or mild cases. Where other safer, lower coast drug can work>
Since the half life for remdesivir to be degraded or metabolized is about 16 hours, its effectiveness could be partly explained by the perturbation on surface membrane proteins. (https://www.frontiersin.org/articles/10.3389/fphar.2020.01091/abstract)
I appreciate researchers who provided suggestions, but the half-life of RSV is about 1 hr , the metabolites monophosphate is relatively polar with poor access to lung tissues. This what i believe now as a pharmacologist. Probably I change my opinion if any college shows evidence of good access to the active metabolite to lung tissues. This not mean no benefit as the virus is disseminated to other organs and immune cells.
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