Ceragenins show promise as a powerful COVID-19 therapy

Efficacy and safety demonstrated in numerous studies

What they are:

Ceragenins are non-peptide small molecule mimics of endogenous antimicrobial peptides. They display broad-spectrum antibacterial, antifungal and antiviral activity against lipid-enveloped viruses including SARS-CoV-2 (COVID-19). In vitro and in vivo studies have established this activity.

Advantages over current therapies:

Breadth of activity against opportunistic pathogens and viruses

Duration of activity

Safety / tolerability

How they are used:

Used as a nebulized, aqueous formulation for prevention and possible treatment of viral infection and secondary bacterial infections in the sinuses and lung. 

Kills COVID-19

Test results for Virucidal Efficacy testing performed at Analytical Lab Group on March 23, 2020.

Dried Virus Control Results:

  • Human Coronavirus = 4.50 log10/100µL (4.80 log10/carrier) 2-minute exposure
  • Human Coronavirus = 4.50 log10/100µL (4.80 log10/carrier) 5-minute exposure

Cytotoxicity Control Results:

  • Lot SL0050 = ≤0.50 log10/100µL
  • Lot SL0050 – 2-minute Exposure: Complete inactivation of the test virus was demonstrated [≤0.50 log10/100µL (≤0.80 log10/carrier)].  A ≥4.00 log10 reduction in viral titer was demonstrated. (PASSED)  
  • Lot SL0050- 5-minute Exposure: Complete inactivation of the test virus was demonstrated [≤0.50 log10/100µL (≤0.80 log10/carrier)].  A ≥4.00 log10 reduction in viral titer demonstrated. (PASSED) 

All test control results met acceptance criteria for a valid test. Test results meet EPA criteria for a virucidal label claim.  

Kills coronaviruses without resistance

Ceragenins formulated in micelles are well tolerated at high concentrations in the lung and trachea while retaining antimicrobial activity. Although anecdotal, the Ceragenin-containing products used for animal care have been used for treatment in the lungs of racehorses for years with good results and no adverse events. In the description of uses of Ceragenin given below, the term CSA refers to these Ceragenin-containing products.

Bacterial counts in the lungs of mice infected with P. aeruginosa that had received tobramycin or ceragenin CSA-13, in nebulized form

Blocks COVID-19

SARS-CoV-2 virus has entry factors that are highly expressed in nasal and bronchial epithelial cells together with innate genes to gain entry into human cells and cause infection. The virus has strong affinity and tropism for the respiratory epithelial cells. Gene array studies show that Ceragenins downregulate expression of IRAK proteins and TNF-α. In addition, Ceragenins modulate the body’s innate immune response against viruses.

Kills secondary infection without resistance and pathogenic fungi – Excellent data showing Viricidal activity to SARS-CoV-2 with Ceragenins.

How they work:

Ceragenins effectively mimic key components of innate immunity, providing continuous protection against pathogens ranging from bacteria to fungi to viruses. The continuity and breadth of activity of innate immunity is essential due to constant exposure to a broad array of pathogens. A key component of innate immunity is endogenous antimicrobial peptides (AMPs). Ceragenins are small-molecule mimics of AMPs and are derived synthetically from a common bile acid.

The activities of Ceragenins have been described in more than 90 peer-reviewed papers.

  • Ceragenins retain activity in the lung even in the presence of lung fluids containing mucins, DNA and F-actin, which inhibit the activities of endogenous AMPs
  • A Ceragenin, administered via nebulization of an aqueous solutions, showed comparable activity to tobramycin in a murine model of Pseudomonas aeruginosa lung infection
  • Ceragenins formulated in micelles are well tolerated at high concentrations in the lung and trachea while retaining antimicrobial activity
  • Ceragenins are water soluble and can be nebulized for inhalation
  • Ceragenins are produced at large scale and because they are not peptide based, they are stable in the presence of proteases
  • Ceragenins represent a class of compounds with several lead compounds – Ceragenins CSA-44 and CSA-131

Safety data in lung on coated endotracheal tubes:

Ceragenins has been safely studied in many in-vitro studies and in-vivo studies and peer reviewed papers have been written about this new technology. Recently Ceragenin coated endotracheal tubes have been evaluated in two pivotal studies and this showed good safety and efficacy as a medical device.

The CSA coated endotracheal tube was designated a “breakthrough device” by the FDA and has recently been granted emergency use authorization in Canada.

Scanning Electron Microscopy (SEM) images of endotracheal uncoated tube and CSA coated tube

Scanning Electron Microscopy (SEM) images of ETT surfaces: A: biofilm of C. auris (CDC 383) on an uncoated tube after 14 days (daily inoculation). B: surface of a coated tube after 14 days (daily inoculation with C. auris). C: mixed species biofilm of MRSA and PA01 on an uncoated tube after 48 h. D: surface of a coated tube after 48 h (inoculation with MRSA and PA01). E: mixed species biofilm of PA01 and C. auris on an uncoated tube after 48 h. F: surface of a coated tube after 48 h (inoculation with PA01 and C. auris).

Ceragenins are proven:

  • Effective against the world’s most dangerous, drug-resistant bacteria including: MRSA, CRE, ESBL, VRE, Drug-Resistant Gonorrhea and many more
  • Effective against viruses including: HIV, Type I & II Herpes, Herpes Zoster (Shingles), SARS-CoV-2 and other lipid-enveloped viruses
  • Effective against fungi including the deadly, drug-resistant Candida auris
  • Effective against cancers even wild types
  • Have selective mode of action, only targeting pathogens, (leaving the microbiome unaffected)
  • Do not engender resistance
  • Accelerates wound healing and tissue repair
  • Binds endotoxins signal cell and migration, crucial in wound repair
  • Mimics Cathelicidins like LL-37 in directing the innate immune system, regulating cytokines, in turn, managing inflammation
  • Increases the efficacy of antibiotics on drug-resistant bacteria strands
  • Stable and scalable

No study to date has shown any related adverse events. 

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Supporting documentation available upon request.