BACKGROUND
Emerging drug resistant and virulent bacterial strains pose a significant threat to modern clinical practice due to increasing pressure on existing antibacterial therapies and the rise in hospital and community-based infections. Multi‐drug resistant (MDR) pathogenic bacteria and fungi are now resistant to most available antibiotics and antifungals, including new generation, ceftazidime and daptomycin. Hence, there is an urgent need for the next generation of antibacterial agents. Our discovery of a new group of small molecules – cyanoximes – followed by their intensive research allowed establishing the foundation for identifying several novel, biologically active compounds, some of which were selected for further development. Several cyanoximes and their derivatives demonstrated pronounced growth-regulating, pesticide detoxifying, antimicrobial and anti-cancer properties. Antimony had already proven to be an important high efficacy element in developing anti-leishmaniasis drugs, such as Pentostam and Glucantine, and therefore was selected as a central atom.
SUMMARY OF TECHNOLOGY
Our group had synthesized and characterized a group of 12+ novel, proprietary compounds that belong to antimony-based small molecules. Having conducted spectroscopic data and crystal structure evaluation of the compounds, we also completed multiple assays that demonstrated efficacy of our new molecules against pathogenic Gram-positive, Gram-negative bacteria and fungi. Some results are presented below.
Antimicrobial activity of compounds A, B and E against Gram-positive MDR bacterium Staphylococcus aureus MRSA NRS70 and fungi Cryptococcus neoformans, and Candida albicans (*, p value <0.01). MIC (µM), S. aureus, A: 146 B: 82 E: 92; C. neoformans, A: 22 B: 37 E: 35; C. albicans, A: 58 B: 54 E: 23.
To build upon our initial proof of concept results and advance our new class of agents towards clinical applications aiming to treat pathogenic bacteria and fungi-related infections, we will pursue preclinical evaluation using in-vivo models and will work to improve the formulation, physicochemical and functional properties of our new compounds for oral delivery.
POTENTIAL AREAS OF APPLICATION
- Development of new non‐antibiotic drugs for multidrug-resistant (MDR) bacteria and fungi
- Mucus‐type antimicrobial hydrophobic additives to adhesives working in aqueous environment
- Antimicrobial wearable sweat resistant electronic devices for electrodes, contact pads
- Antimicrobial polymer glue that sticks to wet surfaces for underwater applications
MAIN ADVANTAGES
- A series of novel, patent-pending compounds
- A new mechanism of action involving Sb-based agents that open the opportunity for optimizing druggability of these compounds
COMMERCIAL OPPORTUNITY
The global antibiotic resistance market size was valued at USD 7.81 billion in 2017 and estimated to have a CAGR of 5.6% from 2018 to 2025. According to GlobalData, the world market for gram-negative bacteria is projected to exceed $3.6 billion by 2026. Pharmaceutical companies are looking for broadly acting antimicrobials, applicable for oral applications. We are seeking partners to help us evaluate and further develop our lead compounds.