# Revising Anti-coronavirus Compounds to Enhance Activity and Optimize Delivery

> **NIH NIH R01** · UNIVERSITY OF CALIFORNIA, SAN DIEGO · 2021 · $766,165

## Abstract

Project Summary/Abstract
The current outbreak of COVID-19 has had devastating global effects on morbidity and
mortality. Currently no vaccine is available and no therapeutic with efficacy against
SARS-CoV-2019 have been fully approved by the FDA. Remdesivir, an intravenous
drug which inhibits the viral RNA polymerase enzyme, has received an EUA designation
by the US FDA. A prodrug of N4-hydroxy-cytidine has recently entered Phase 1 trials.
Our goal is to synthesize COVID-19 antivirals that inhibit the viral RNA polymerase and
can be used orally or intramuscularly with a special focus on delivering maximal
amounts of drug to the lungs.
We will synthesize prodrugs of remdesivir and other nucleosides with anti-coronavirus
activity using an innovative approach that involves converting them to lipid analogs.
Some compounds will focus on oral delivery and others on intramuscular administration.
The compounds will be screened in vitro against nonpathogenic and pathogenic
coronaviruses including SARS-CoV-2 and their activity compared with the unmodified
parent nucleosides. Their pharmacokinetics and toxicity of the most active antivirals will
be studied in rats. The active antivirals will be evaluated for exposure to lung versus
their unmodified nucleosides. Finally, the clinical and antiviral activity of the most
promising compounds will be evaluated in the Syrian Golden hamster model of
coronavirus disease.

## Key facts

- **NIH application ID:** 10240178
- **Project number:** 1R01AI161348-01
- **Recipient organization:** UNIVERSITY OF CALIFORNIA, SAN DIEGO
- **Principal Investigator:** Karl Y Hostetler
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $766,165
- **Award type:** 1
- **Project period:** 2021-09-01 → 2024-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10240178

## Citation

> US National Institutes of Health, RePORTER application 10240178, Revising Anti-coronavirus Compounds to Enhance Activity and Optimize Delivery (1R01AI161348-01). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10240178. Licensed CC0.

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