RESEARCH TRIANGLE PARK – RedHill Biopharma, an Israeli company with U.S. headquarters in Raleigh, says one of its drug candidates, opaganib, completely inhibited the replication of the coronavirus that causes COVID-19 in a laboratory study.

Preliminary results showed that opaganib had “a clear and compelling antiviral effect” against  the SARS-CoV-2 virus and demonstrated the most potent activity compared to all compounds tested, including the positive control, remdesivir, a treatment commonly used for COVID-19, the company reported.

“Opaganib’s previously demonstrated anti-inflammatory activity, combined with our now proven specific anti-SARS-CoV-2 viral activity, provides a unique dual mechanism of action with the potential to greatly benefit COVID-19 patients by inhibiting the key drivers of disease progression — viral replication and lung inflammation,” said Mark L. Levitt, M.D., Ph.D., medical director at RedHill.

The positive study data support RedHill’s goal of “generating a robust data package to potentially support emergency use authorization” of opaganib for treating COVID-19, Levitt said.

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Working with the University of Louisville Center for Predictive Medicine, RedHill studied the efficacy of opaganib in a three-dimensional tissue model of human bronchial epithelial cells. The model, called EpiAirway, resembles the form and function of the human airway and is similar to the model used to discover SARS-CoV-2.

Treatment of cells infected with SARS-CoV-2 completely inhibited virus production, as measured after three days of incubation, without compromising cell membrane integrity, a measure of cell viability and drug safety, according to RedHill.

Data from the pre-clinical study will be submitted to a peer-reviewed journal, the company reported.

Clinical trials under way

Opaganib, branded under the registered name Yeliva, is a first-in-class, orally administered, sphingosine kinase-2 selective inhibitor. It has dual anti-inflammatory and anti-viral activity that targets a host cell component and is unaffected by viral mutation, thus minimizing the likelihood of drug resistance.

Opaganib is being evaluated in global Phase 2/3 and U.S. Phase 2 clinical studies for the treatment of severe COVID-19 pneumonia.

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The global study continues to enroll up to 270 patients requiring hospitalization and treatment with supplemental oxygen. The study recently received approval in Israel and has been approved in the United Kingdom, Italy, Russia and Mexico.

The U.S. Phase 2 study will enroll up to 40 patients requiring hospitalization and supplemental oxygen. It is more than 50 percent enrolled, the company reported.

Opaganib, a new chemical entity, has anticancer, anti-inflammatory and antiviral activities, and is being investigated for multiple oncology, viral, inflammatory and gastrointestinal indications. It received Orphan Drug designation from the U.S. Food and Drug Administration for the treatment of cholangiocarcinoma, a rare cancer of the bile ducts, and is being evaluated in a Phase 2a study in advanced cholangiocarcinoma and in a Phase 2 study in prostate cancer.

Another potential COVID-19 drug progressing

In addition to opaganib, RedHill’s pre-clinical study evaluated the antiviral activity of another investigational drug, upamostat, a serine protease inhibitor.

Results demonstrated “potent inhibition” of SARS-CoV-2 viral replication, the company reported, and a U.S. Phase 2/3 study of upamostat in an outpatient setting is planned to begin later this year.

“As with opaganib, upamostat is orally bioavailable and therefore potentially suitable for both inpatient and out-patient settings,” said Terry F. Plasse, M.D., medical director at RedHill.

RedHill, established in 2009 in Tel Aviv, is a specialty biopharmaceutical company focused on the treatment of gastrointestinal diseases. RedHill’s sales team, based in Raleigh, promotes three gastrointestinal products in U.S. markets: Talicia, Movantik and Aemcolo.

The company’s shares are publicly traded on the NASDAQ stock market and the Tel Aviv Stock Exchange.

(C) N.C. Biotech Center