Updates on development of oral remdesivir formulations

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Jubilant Pharmova subsidiary Jubilant Pharma has concluded safety and pharmacokinetic/absorption studies of a new oral formulation of remdesivir in animals and healthy human volunteers in India. The novel formulation can potentially lower the capacity constraint faced by the injectable form of remdesivir and guarantee broader and timely availability for the patients. The oral formulation is designed to side-step hepatic metabolism, which causes complete first-pass elimination of the drug when administered orally through traditional means. According to the latest findings from both preclinical and human studies, remdesivir was shown to undergo absorption on administering as an oral formulation. Furthermore, oral remdesivir was observed to be well tolerated in all the study subjects with no new safety/ tolerability issues when compared to the injectable dose.

The Food and Drug Administration approved the use of Redesivir i.v. in October 2020 and it remains the only FDA-approved antiviral for treatment of SARS-CoV-2 infection.

An oral version of remdesivir is being developed by scientists at the University of California, San Diego (UCSD) to combat the SARS-CoV-2 virus early in its infection cycle published recently in Antimicrobial Agents and Chemotherapy. Though still in preclinical trials, results suggest it could reduce disease severity and hospitalizations thanks to its longer half-life, greater efficacy and reduced toxicity when compared to remdesivir. The most active of the three oral lipid prodrugs the researchers developed, ODBG-P-RVn, is eight times more active than remdesivir in Vero E6 cells and as effective as remdesivir in the other cell types tested.  

Gilead is also working on development of oral remdesivir version, which is a nucleosid of the active metabolite: the in vitro antiviral activity and in vivo therapeutic efficacy of GS-621763, an orally bioavailable prodrug of GS-441524, the parental nucleoside of remdesivir, which targets the highly conserved RNA-dependent RNA polymerase. GS-621763 exhibited significant antiviral activity in lung cell lines and two different human primary lung cell culture systems.

While the i.v. formulation (having FDA approval) was formulated with SBECD, the oral formulation is a lipid prodrug with no CD.

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