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Sunday, May 02, 2021 12:05:35 PM
Defensin-based therapeutics—of which Brilacidin is the leading example, and the most advanced drug candidate among this class currently in clinical testing—represent an attractive possible intervention to combat the coronavirus given innate and multifaceted immunomodulatory properties. Defensins exhibit a number of distinct and highly favorable therapeutic characteristics: anti-bacterial, anti-inflammatory, anti-fungal, anti-biofilm, anti-cancer, and antiviral.
Brilacidin, a mimetic of defensins, was computationally designed to be smaller (1/10th the size), more stable, more potent (by a 100-fold) and more selective (by a 1000-fold) than natural defensins, a type of antimicrobial peptide, so as to overcome most shortcomings (e.g., degradation, toxicity, malabsorption, high-cost of manufacturing) that have complicated their clinical development. The antiviral properties of natural defensins and their synthetic mimics are actively being studied by virologists the world over, with newer understandings elucidating their direct mechanisms of action against non-enveloped and enveloped viruses alike, along with their role in the regulation of inflammation and chemoattraction.
http://www.ipharminc.com/press-release/2020/3/2/innovation-pharmaceuticals-provides-scientific-rationale-and-clinical-development-perspectives-for-brilacidin-as-a-potential-novel-coronavirus-covid-19-treatment
...based on molecular screening of 11,552 compounds comprising already FDA-approved drugs and those in clinical testing, Brilacidin, the Company’s defensin-mimetic drug candidate targeting COVID-19, was identified as one of the most promising potential inhibitors of SARS-CoV-2, the novel coronavirus responsible for COVID-19. The researchers who conducted the study concluded: “Clearly, these compounds should be further evaluated in experimental assays and clinical trials to confirm their actual activity against the disease.”
http://www.ipharminc.com/press-release/2020/4/20/screening-of-11552-compounds-identifies-innovation-pharmaceuticals-brilacidin-as-one-of-the-most-promising-potential-inhibitors-of-the-novel-coronavirus
Brilacidin, in an in vitro experiment using VERO cells, reduced the viral titer (load) of SARS-CoV-2 by 75 percent after only 1 hour of preincubation prior to infection at a concentration of 10µM as compared to vehicle control.
These statistically significant lab results strongly support Brilacidin’s prophylactic treatment potential given the drug’s potent and rapid virucidal activity—a unique ability, different from any other known drug currently in development to treat COVID-19, to inactivate the novel coronavirus prior to host cell entry and subsequent viral replication. A majority of antiviral agents targeting SARS-CoV-2 attempt to inhibit viral replication rather than completely eliminating the virus (virustatic versus virucidal).
http://www.ipharminc.com/press-release/2020/5/19/innovation-pharmaceuticals-brilacidin-reduces-viral-titer-of-sars-cov-2-covid-19-by-75-percent-after-only-1-hour-of-preincubation-in-in-vitro-study-at-bsl-3-facility
Brilacidin exhibited a statistically significant (p<0.0001) and potent inhibitory effect on SARS-CoV-2, the novel coronavirus responsible for COVID-19, in a human lung epithelial cell line—reducing viral load by 95 percent and by 97 percent, compared to control, at two therapeutic concentrations tested. Based on a CC50 value—the concentration of drug at which 50 percent of cells maintain viability—Brilacidin was also shown to be non-cytotoxic in the lung cell line.
http://www.ipharminc.com/press-release/2020/6/17/innovation-pharmaceuticals-brilacidin-inhibits-sars-cov-2-covid-19-by-97-percent-in-a-human-lung-cell-line
[The primary investigator at the RBL noted that the human lung cell experiments reflect a similarly robust in vitro antiviral signal against SARS-CoV-2 as assessed in vero cells (animal), with Brilacidin showing consistent demonstration of efficacy across different cell lines. Brilacidin also appears to be showing greatest efficacy in testing when administered as a pre-treatment (virus pre-incubated with Brilacidin prior to infection), in addition to being present during and post-infection.
http://www.ipharminc.com/press-release/2020/7/7/in-vitro-testing-of-innovation-pharmaceuticals-brilacidin-for-covid-19-shows-consistent-anti-sars-cov-2-efficacy-manufacturing-preparation-underway-for-covid-19-clinical-trial
Brilacidin exhibited a similarly potent inhibitory effect against SARS-CoV-2 at an even lower concentration in the same human lung epithelial cell line. Brilacidin achieved approximately 90 percent inhibition of SARS-CoV-2 at a drug concentration that was one-half lower than previously tested. The lowest concentration of Brilacidin used in RBL testing to date is well below the clinically-achievable concentration based on the pharmacokinetics observed in the Company’s Phase 2b clinical trial of Brilacidin in Acute Bacterial Skin and Skin Structure Infections.
http://www.ipharminc.com/press-release/2020/7/20/innovation-pharmaceuticals-brilacidin-inhibits-novel-coronavirus-covid-19-by-almost-90-at-the-lowest-concentration-tested-to-date-in-a-human-lung-cell-line
“Selectivity Index is arguably the most important measure to compare the antiviral efficacy between experimental drugs and this new data suggests Brilacidin [SI=426] is in an elite group of anti-coronavirus candidates. For a point of reference, a SI greater than 100 is considered exceptional. Unlike thousands of other compounds and drugs under consideration as COVID-19 treatments, Brilacidin is demonstrating remarkably consistent and potent anti-SARS-CoV-2 activity in RBL testing, suggesting Brilacidin has tremendous potential as a COVID-19 treatment.
http://www.ipharminc.com/press-release/2020/8/24/covid-19-drug-candidate-brilacidin-achieves-a-selectivity-index-among-the-highest-reported-exhibiting-potent-anti-sars-cov-2-activity-at-low-concentrations-clinical-trial-forthcoming
...the U.S. Food and Drug Administration (FDA) has designated as a Fast Track development program the investigation of Brilacidin as a potential treatment for COVID-19. Brilacidin is a first-in-class Host Defense Protein (HDP) mimetic with antiviral, anti-inflammatory and antibacterial properties.
http://www.ipharminc.com/press-release/2021/1/14/innovation-pharmaceuticals-brilacidin-for-the-treatment-of-covid-19-receives-fda-fast-track-designation
The Company is highly encouraged by this independent research suggesting Brilacidin may be one of the best drug candidates capable of attacking and destroying SARS-CoV-2 variants and other coronaviruses, while mitigating or averting the threat of drug resistance developing.
http://www.ipharminc.com/press-release/2021/3/10/innovation-pharmas-covid-19-drug-candidate-brilacidin-ranked-in-top-three-percent-of-compounds-predicted-to-be-most-effective-against-sars-cov-2
Dr. Narayanan has been leading ongoing research assessing Brilacidin’s broad spectrum antiviral potential, with preliminary in vitro data showing Brilacidin potently inhibits both coronaviruses and alphaviruses. As previously released, these data will serve as the basis for an Oral Presentation on Brilacidin’s antiviral properties to be delivered at the American Society of Virology’s 40th Annual Meeting (ASV 2021), taking place July 19-23, 2021.
http://www.ipharminc.com/press-release/2021/4/14/innovation-pharmas-broad-spectrum-antiviral-drug-candidate-brilacidin-highlighted-in-biodefense-and-infectious-diseases-covid-19-presentation
If one can't be hopeful about B-COVID's chances for EUA approval with this mountain of evidence then maybe a little fluoxetine is in order.
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