Remdesivir, is a broad-spectrum antiviral medication.
Administered intravenously as a pro drug that inhibits viral RNA polymerase.
The active metabolite of remdesivir is an adenosine nucleoside triphosphate analog that interferes with the action of viral RNA-dependent RNA polymerase and evades proofreading by viral exoribonuclease, causing a decrease in viral RNA production.
A nucleotide analog prodrug that inhibits the viral RNA dependent RNA polymerase and approved for adults in select pediatric patients with severe Covid-19 who require hospitalization.
In a randomized trial in participants at high risk for progression, it reduced hospitalization, or death by 87% compared with placebo.
It is approved for adult and pediatric patients 28 days of age and older, weighing at least 3 kg and who are at higher risk for progression to severe Covid, and within seven days of symptom onset.
The medication is administered once daily for three days.
Brand name Veklury.
It is administered via intravenous injection.
Approved or authorized for emergency use to treat COVID‑19.
World Health Organization in November 2020 had a conditional recommendation against the use of remdesivir for the treatment of COVID-19.
Pregnancy category US: N (Not classified yet).
Common side effect in healthy volunteers is raised LFTs.
The most common side effects in people with COVID‑19 is nausea.
Side effects may include liver inflammation and an infusion-related reaction with nausea, low blood pressure, and sweating.
It is a prodrug that is intended to allow intracellular delivery of monophosphate and subsequent biotransformation into triphosphate, a ribonucleotide analogue inhibitor of viral RNA polymerase.
The most common adverse effects: include respiratory failure and organ impairment, low albumin, low potassium, low count of red blood cells, low count of platelets that help with clotting, and jaundice, gastrointestinal distress, elevated transaminase levels and infusion related and site reactions.
Infusion‐related reactions may include: low blood pressure, nausea, vomiting, sweating, and shivering.
Increases in levels of liver enzymes in patients that have received remdesivir.
NIAID-ACTT study suggested a beneficial effect of remdesivir in the treatment of hospitalized individuals with severe COVID‑19.
Remdesivir is a prodrug and is able to achieve its active metabolite triphosphate by nucleoside-phosphate kinases.
As an adenosine nucleoside triphosphate analog.
In some viruses such as the respiratory syncytial virus it causes the RNA-dependent RNA polymerases to pause, but its main effect is to induce an irreversible chain termination.
It delays the addition of subsequent nucleotides, after five additional bases have been added to the growing RNA chain.
Classified as a direct-acting antiviral agent that works as a delayed chain terminator.
It is at least partially metabolized by the cytochrome P450 enzymes CYP2C8, CYP2D6, and CYP3A4, and concentrations of remdesivir are expected to decrease if it is administered together with cytochrome P450 inducers such as rifampicin, carbamazepine, phenobarbital, phenytoin, primidone, and St John’s wort.
Using chloroquine or hydroxychloroquine with remdesivir may reduce the antiviral activity of remdesivir.
Coadministration of remdesivir and chloroquine phosphate or hydroxychloroquine sulfate is not recommended, as data demonstrating an antagonistic effect of chloroquine on the intracellular metabolic activation and antiviral activity of remdesivir.
Its manufacturing requires 70 raw materials, reagents, and catalysts to make, and approximately 25 chemical steps.
Some of its ingredients are extremely dangerous to humans, especially trimethylsilyl cyanide.
In a double-blind, placebo-controlled clinical trial looked at 1,062 hospitalized subjects with mild, moderate and severe COVID‑19 who received remdesivir or placebo plus standard of care.
The median time to recovery from COVID‑19 was 10 days for the remdesivir group compared to 15 days for the placebo group, a statistically significant difference.
In a second randomized, open-label multi-center clinical trial of hospitalized adult subjects with moderate COVID‑19 compared treatment with remdesivir for five days and treatment with remdesivir for 10 days with standard of care.
Among non-hospitalized patients who were at high risk for Covid-19 progression a three day course of remdesevir had an acceptable safety profile and resulted in an 87% lower risk of hospitalization or death than placebo.
According to international experts from the British Medical Journal: probably has no important effect on the need for mechanical ventilation and may have little or no effect on the length of hospital stay.
It is likely that it has a clinical benefit for Covid-19 patients before hospitalization then later in the course of disease.
Has efficacy in Ebola infections.