# Optimization of orally bioavailable inhibitors for the treatment of COVID-19 and other human coronavirus infections

> **NIH NIH R44** · VENATORX PHARMACEUTICALS, INC. · 2024 · $1,000,000

## Abstract

PROJECT SUMMARY
The emergence of SARS-CoV-2 in 2019 has resulted in an ongoing epidemic of acute respiratory illness that
has stressed the world’s health care systems and led to >6 million deaths. The lack of therapeutic options for
treating coronavirus infections continues to expose the population to grave risk from emerging variants as well
as future zoonotic coronavirus infections. Accelerated drug discovery/development techniques, including drug
repurposing and fast follower drug design have only resulted in the approval of a single orally bioavailable
inhibitor. Nirmatrelvir/Paxlovid is contraindicated in a large fraction of patients, susceptible to emerging
resistant variants and may not demonstrate cross-activity against future coronavirus threats. Therefore, future
efforts should focus on the development of new antivirals including those that possess complementary
mechanisms of action and resistance profiles. During this Phase 2 project, we will execute a medicinal
chemistry/profiling strategy and complete optimization of a novel series of SARS-CoV-2 entry inhibitors to
improve their antiviral activity against SARS-CoV-2 and other coronaviruses as well as their pharmacokinetic
properties. The overall goal of this project is to select a Development Candidate for the treatment of COVID-19
and ready the compound for IND-enabling GLP toxicity studies.

## Key facts

- **NIH application ID:** 10860995
- **Project number:** 5R44AI177015-02
- **Recipient organization:** VENATORX PHARMACEUTICALS, INC.
- **Principal Investigator:** Glen Coburn
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $1,000,000
- **Award type:** 5
- **Project period:** 2023-06-07 → 2026-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10860995

## Citation

> US National Institutes of Health, RePORTER application 10860995, Optimization of orally bioavailable inhibitors for the treatment of COVID-19 and other human coronavirus infections (5R44AI177015-02). Retrieved via AI Analytics 2026-05-28 from https://api.ai-analytics.org/grant/nih/10860995. Licensed CC0.

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