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Brilacidin COVID-19 Therapeutic

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Last reviewed
June 23, 2022
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Brilacidin Antiviral Description

Innovation Pharma Brilacidin is a Host Defense Protein (HDP) mimetic representing a new drug class with antiviral, anti-inflammatory, and anti-bacterial properties. Brilacidin (PMX-30063) is a synthetic, non-peptidic small molecule that kills pathogens swiftly, significantly reducing drug resistance development. Brilacidin also functions in a robust immunomodulatory capacity, lessening inflammation, and promoting healing. In addition, Brilacidin has the potent ability to inhibit coronaviruses, primarily by disrupting viral integrity and blocking viral entry.

Modeled after HDPs, the "front-line" of defense in the body's innate immune system is a synthetic, non-peptidic small-molecule module that kills pathogens swiftly, significantly reducing the likelihood of drug resistance developing. In addition, laboratory testing at independent laboratories supports Brilacidin's antiviral ability to safely and potently inhibit SARS-CoV-2 and multiple strains of human coronaviruses. For example, in a human lung cell line against the SARS-CoV-2 betacoronavirus, Brilacidin achieved a Selectivity Index of 426.

Brilacidin and related compounds are protected under various compositions and use patents. For example, a patent was filed and is pending for HDP-mimetics in the prevention and/or treatment of inflammatory diseases of the gastrointestinal tract. Another patent for compounds for use in the treatment of mucositis has been awarded numerous global protections—additionally, an oral rinse containing brilacidin, a defensin mimetic, with potential antimicrobial and anti-mucositic activities. Defensins are a major class of antimicrobial peptides active against a broad spectrum of microbes, including various enveloped and non-enveloped viruses.

The U.S. FDA granted IND Approval for Phase 2 Clinical Trial for Brilacidin treating COVID-19 in December 2020. On February 9, 2021, the journal Cell Culture published a paper that concluded Brilacidin was shown to exert potent inhibitory effects on SARS-CoV-2 in cell culture by decreasing viral load in different cell types, including ACE2 positive human lung cells and, notably, in both the Washington and Italian strains of the coronavirus. Brilacidin has been granted U.S. FDA Fast Track designation and is currently being evaluated in a randomized, placebo-controlled Phase 2 clinical trial in hospitalized COVID-19 patients: Last Update Posted: August 13, 2021.

The Company has received individual patient Expanded Access (compassionate use) requests for Brilacidin to treat critically ill COVID-19 patients who are not responding to prior therapy. Following receipt of such requests, the Company has supplied Brilacidin to relevant hospitals for individual patient use. In addition, the U.S. FDA granted treating physicians permission to administer Brilacidin.

A Research Article published on January 25, 2022 - Brilacidin, a COVID-19 drug candidate, demonstrates broad-spectrum antiviral activity against human coronaviruses OC43, 229E, and NL63 through targeting both the virus and the host cell - this study provides appealing findings for the translational potential of brilacidin as a broad-spectrum antiviral for coronaviruses including SARS-CoV-2. And on March 15, 2022, Brilacidin was shown to exert a dual-acting antiviral mechanism of action, able to target coronaviruses directly and bind to host cell surfaces to prevent viral entry. In addition, on June 23, 2022, the Company announced its defensin-mimetic drug candidate inhibited the Omicron (B.1.1.529) and Delta (B.1.617.2) variants of SARS-CoV-2 based on in vitro testing conducted in collaboration with the National Institutes of Health (NIH) National Institute of Allergy and Infectious Diseases scientists.

ChemSpider ID: 28651526; Formula: C40H50F6N14O6; PubChem CID: 25023695; Brilacidin EPA: 1224095-98-0 | DTXSID90153594

Innovation Pharma is developing Brilacidin for COVID-19 under Fast Track designation from the FDA. Given the need for the development of new small-molecule antivirals and immunomodulators, as of early March 2022, the Company is planning to submit Brilacidin for possible inclusion in government-sponsored COVID-19 trial platforms, e.g., the NIH ACTIV program.

Headquartered in Wakefield, Massachusetts, Innovation Pharmaceuticals Inc. (formerly Cellceutix Corporation) is a publicly-traded biopharmaceutical company (OTCQB: IPIX) dedicated to discovering and advancing innovative medical therapies in dermatology, oncology, anti-inflammatory, antibiotic, and antiviral applications.

Brilacidin History

Innovation Pharma is developing Brilacidin for COVID-19 under Fast Track designation from the U.S. FDA. Upon recently completing a scheduled review of interim safety data from the trial, an independent Data Monitoring Committee recommended increasing the dosing regimen of Brilacidin from 3 days to 5 days of treatment, which may maximize therapeutic benefits and provide a comparison with 5-day remdesivir (Veklury), currently the only FDA-approved treatment for COVID-19. Accordingly, on December 21, 2020, Innovation Pharmaceuticals announced that the U.S. FDA had approved the Company's Investigational New Drug application to initiate a Phase 2 clinical trial.

Click here for a bibliography on the development of Brilacidin and the HDP-mimetics program. Brilacidin was evaluated as an ocular anti-infective in 2016.

Brilacidin Indication

Brilacidin COVID-19 therapeutic candidate is a broad-spectrum antiviral for treating common colds and coronavirus infections. Brilacidin is an antibiotic that disrupts bacterial cell membranes, mimicking defensins that play a role in innate immunity. Upon rinsing with the brilacidin oral rinse, bacterial cell membrane lysis and leakage of cellular cytoplasmic contents. This inhibits bacterial activity and may prevent or treat radiation-induced mucositis. Defensins, a family of antimicrobial and cytotoxic peptides expressed mainly by epithelial cells and neutrophils, play a key role in the natural human innate immunity against pathogens.

Upon rinsing with the brilacidin oral rinse, brilacidin imitates defensin as a human HDP and binds to and disrupts the bacterial cell membrane. This causes bacterial cell membrane lysis and leakage of cellular cytoplasmic contents. This inhibits bacterial activity and may prevent or treat radiation-induced mucositis. Defensins, a family of antimicrobial and cytotoxic peptides expressed mainly by epithelial cells and neutrophils, play a key role in the natural human innate immunity against pathogens.

Brilacidin Oral Rinse

An oral rinse containing brilacidin, a defensin mimetic, with potential antimicrobial and anti-mucositic activities. Upon rinsing with the brilacidin oral rinse, brilacidin imitates defensin as a human host defense protein (HDP) and binds to and disrupts the bacterial cell membrane. This causes bacterial cell membrane lysis and leakage of cellular cytoplasmic contents. This inhibits bacterial activity and may prevent or treat radiation-induced mucositis.

Brilacidin News For 2020 - 2022

June 23, 2022 - Innovation Pharma confirmed that Brilacidin has now been tested in vitro in seven SARS-CoV-2 strains (Omicron, Delta, Gamma, Alpha, Italian, Washington, Wuhan) and three human coronaviruses (H-CoV) strains (OC43, 229E, and NL63), in addition to MERS-CoV and SARS-CoV-1. Brilacidin has consistently inhibited all coronaviruses tested, independent of cell type, at generally attainable systemic concentrations (based on established human pharmacokinetics of IV-administered Brilacidin).

March 15, 2022 - Innovation Pharmaceuticals announced the publication of a peer-review scientific article in the Journal of Medical Virology on the anti-coronavirus properties of Brilacidin. Brilacidin was shown to exert a dual-acting antiviral mechanism of action, able to target coronaviruses directly and bind to host cell surfaces to prevent viral entry.

March 7, 2022 - Innovation Pharmaceuticals reported findings from a data review of the Company's Brilacidin Phase 2 COVID-19 study and compassionate use of Brilacidin in critically-ill COVID-19 patients.

November 18, 2021 - The Company is further encouraged by the compassionate use of Brilacidin, which involved treating extremely critically ill patients who had exhausted all other therapeutic options. Compassionate use cases comprised Brilacidin being administered over a longer duration (up to 10 days) than in Phase 2 COVID-19 trial (3 and 5-day dosing), with some patients also receiving higher and more frequent dosing (two doses every 24 hours). Patient data is planned to be compiled and evaluated, which may shed additional light on Brilacidin's treatment potential in COVID-19.

November 12, 2021 - New in vitro data also show Brilacidin targets both viral proteins and host factors, suggesting Brilacidin would be less prone to developing resistance compared to other antivirals.

September 23, 2021 - Innovation Pharmaceuticals provided an update on the status of its randomized, double-blind, placebo-controlled Phase 2 clinical trial of Brilacidin. Based on information received from the data management and biostatistics vendors, study unblinding, analysis of the unblinded data, and release of topline study results for the Brilacidin COVID-19 trial is anticipated to occur in mid-to-late October 2021.

August 12, 2021 - Innovation Pharmaceuticals (OTCQB: IPIX) provided additional information regarding the status of its randomized, double-blind, placebo-controlled Phase 2 clinical trial of Brilacidin for the treatment of moderate-to-severe COVID-19 in hospitalized patients (NCT04784897). The Company is developing Brilacidin for the treatment of COVID-19 under the U.S. FDA Fast Track designation. "Our team is as excited as anyone to learn the results of our Brilacidin COVID-19 clinical trial. Everything is advancing per industry norms and standards," said Leo Ehrlich, CEO at Innovation. "We look forward to sharing Brilacidin topline data in treating COVID-19 as soon as we have it in hand."

August 2, 2021 - Innovation Pharmaceuticals provided an update on ongoing antiviral research of Brilacidin, the Company's defensin-mimetic drug candidate being developed for the treatment of COVID-19 under FDA Fast Track designation by different groups of scientists.

July 22, 2021 - Innovation Pharmaceuticals announced that new Brilacidin antiviral data, based on research conducted by George Mason University / National Center for Biodefense and Infectious Diseases researchers, was presented yesterday, July 21, 2021, at the American Society of Virology's 40th Annual Meeting. "Brilacidin continues to show a consistent ability in the laboratory to inhibit different contagious viruses, regardless of viral strain and in a cell type-independent manner," said Aarthi Narayanan, Ph.D., Primary Investigator of Brilacidin at GMU. "Our scientific team looks forward to exploring Brilacidin further as we investigate the breadth of its antiviral profile."

May 13, 2021 - Innovation Pharmaceuticals (OTCQB: IPIX) announced the filing of its SEC Form 10-Q for the quarter that ended March 31, 2021. During the quarter, the Company made substantive progress in developing Brilacidin, Innovation Pharma's flagship drug candidate in a new class of compounds called defensin-mimetics.

April 28, 2021 - Innovation Pharmaceuticals announced that enrollment had surpassed 50 percent of the total targeted number of randomized trial participants (~n=120) in its double-blind, placebo-controlled Phase 2 clinical trial of Brilacidin for treatment of moderate-to-severe COVID-19 in hospitalized patients.

April 14, 2021 - Innovation Pharmaceuticals announced that Brilacidin, the Company's defensin-mimetic drug candidate, was featured in the "Mason Science Series: Rising to the National and International COVID-19 Challenge," a presentation of George Mason University. And in the article published by the journal Nature: 'The race for antiviral drugs to beat COVID — and the next pandemic.'

April 5, 2021 - Innovation Pharmaceuticals announced an independent Data Monitoring Committee (DMC) completed its scheduled review of interim safety data in the Company's randomized, double-blind, placebo-controlled Phase 2 clinical trial of Brilacidin for treatment of moderate-to-severe COVID-19 in hospitalized patients. Recruitment was paused upon reaching 25 percent enrollment (30 subjects), and the DMC conducted a pre-specified unblinded safety data review and evaluation. Following their review, the DMC recommended increasing the dosing regimen of Brilacidin from 3 days to 5 days of treatment, as intended per the protocol, which the Company has since implemented. Recruitment for the 5-day treatment regimen has begun. Efficacy data was not reviewed by the DMC and remained blinded.

March 10, 2021 - Innovation Pharmaceuticals reported that a Machine Learning (Artificial Intelligence) model used to screen 1,482 compounds ranked Brilacidin in the top three percent of compounds predicted to be the most effective against SARS-CoV-2, the virus responsible for COVID-19.

March 2, 2021 - Innovation Pharmaceuticals announced a peer-reviewed scientific article—Brilacidin Demonstrates Inhibition of SARS-CoV-2 in Cell Culture—in the journal Viruses. Leo Ehrlich, Chief Executive Officer of Innovation Pharmaceuticals, commented, "Infectious disease experts have noted the next phase in the global fight against COVID-19 will be in developing potent antivirals that directly act on the SARS-CoV-2 virus—which is what Brilacidin has been shown to do in pre-clinical studies."

February 26, 2021 - Innovation Pharmaceuticals provided additional study details for its ongoing Phase 2 clinical trial assessing Brilacidin as a novel therapeutic in hospitalized patients with COVID-19. Patients are being treated, with recruitment and enrollment progressing at trial sites.

February 9, 2021 - A new review found Brilacidin's anti-SARS-CoV-2 activity 'suggests that SARS-CoV-2 inhibition in these cell culture models is likely to result from the impact of brilacidin on viral entry and its disruption of viral integrity. Brilacidin demonstrated synergistic antiviral activity when combined with remdesivir. Collectively, our data demonstrate that brilacidin exerts potent inhibition of SARS-CoV-2 against different strains of the virus in cell culture.'

January 14, 2021 - Innovation Pharmaceuticals' Brilacidin for the Treatment of COVID-19 Receives FDA Fast Track Designation. Laboratory testing at independent laboratories supports Brilacidin's antiviral ability to safely and potently inhibit SARS-CoV-2 and multiple strains of human coronaviruses. In a human lung cell line against SARS-CoV-2, Brilacidin achieved a Selectivity Index of 426. A molecular screening study of 11,552 compounds also supports Brilacidin as a promising novel coronavirus treatment. Brilacidin antiviral research to date has been limited to laboratory-based experiments.

December 21, 2020 - The U.S. FDA Granted IND Approval for Phase 2 Clinical Trial of Innovation Pharmaceuticals' Brilacidin for Treating COVID-19. Brilacidin's potent in vitro inhibition of the Washington and Italian strains of SARS-CoV-2 supports its potential to inhibit emerging coronavirus mutations (variants), such as those in the United Kingdom, Denmark, and South Africa.

November 30, 2020 - Innovation Pharmaceuticals COVID-19 Clinical Trial to Support Additional Development of Brilacidin as a "Pan-Coronavirus" Therapeutic. Additional independent preliminary laboratory research suggests Brilacidin, the Company's flagship defensin mimetic, can treat other endemic human coronaviruses (H-CoVs), such as those causing common colds, and not just SARS-CoV-2, the novel coronavirus responsible for the ongoing global COVID-19 pandemic.

November 16, 2020 -  Innovation Pharmaceuticals announced that an overseas Clinical Trial Application had been submitted to the governing health agency, with a U.S. Investigational New Drug application submitted this week to the FDA. Both these submissions are part of final preparations for the Company's multinational Phase 2 clinical trial of Brilacidin for COVID-19, which is on track to commence in 2020 upon gaining required approvals.

October 30, 2020 -  Innovation Pharmaceuticals and George Mason University's National Center for Biodefense and Infectious Diseases jointly announced the completion of extensive laboratory testing supporting the anti-SARS-CoV-2 activity of Brilacidin, a defensin-mimetic drug candidate, which is being developed as a potential COVID-19 treatment. "In testing at GMU's BSL-3 lab, we showed that Brilacidin potently inhibits SARS-CoV-2 in vitro against the live virus. Beyond exhibiting treatment potential for those already infected by COVID-19, Brilacidin's ability to disrupt viral integrity and block viral entry indicates it has the added potential to prevent infection, upon appropriate formulation, as a prophylactic. I look forward to working with Innovation to investigate further Brilacidin's antiviral properties," said Aarthi Narayanan, Ph.D., Associate Professor of Systems Biology in Mason's College of Science.

Brilacidin COVID-19 Antiviral Clinical Trial

Clinical Trial NCT04784897: A Study to Evaluate the Efficacy and Safety of Brilacidin in Hospitalized Participants With COVID-19 - This Phase 2 study is a randomized, blinded, placebo-controlled, parallel-group design. The target population to be treated are 120 patients with moderate to severe COVID-19, SARS-CoV-2 infection confirmed by positive standard polymerase chain reaction (PCR) test (or equivalent/ other approved diagnostic test) within 4 days before starting study treatment, and hospitalized with respiratory distress but not yet requiring high-level respiratory support. Last updated on August 13, 2021.

Clinical Trials

No clinical trials found