Reinach, Switzerland, 10 September 2012 – Evolva Holding SA (SIX: EVE) presented extensive preclinical data on EV-035 at ICAAC, the world’s premier international conference on antimicrobial agents and infectious diseases. Professor Jutta Heim, CSO of Evolva, was invited by an ASM expert panel to summarise EV-035 as one of the key new compounds in the oral “Poster Summary Session” at ICAAC on Sunday. Preclinical data on the compound show a broad spectrum of activity against some of the most challenging bacteria, sometimes referred to as ‘Superbugs’. The four discussed posters will be available on Evolva’s website.
In vitro and in vivo data show the compound boasts strong efficacy in combatting bacteria that have become resistant to many of the older generations of antibiotics. The compound’s spectrum includes both Gram-positive and Gram-negative strains, including those resistant to quinolones. EV-035 is particularly potent against Enterococcus, Pseudomonas, Burkholderia and Staphylococcus. In preclinical MRSA models, oral doses of the compound reduced the number of bacteria by 5-6 logs in 24 hours, compared with 2.7 and 2.3 logs for intravenous vancomycin and ciprofloxacin (currently marketed antibiotics), respectively. MRSA (methicillin-resistant Staphylococcus aureus) is a particularly dangerous bacterium as it has developed resistance to almost all current antibiotics. ADMET data reveal EV-035 as well tolerated with no adverse effects in preclinical safety parameters. Good oral bioavailability and a large volume of distribution (in mouse models) warrant exploitation of EV-035 in major bacterial disease indications, including those of intracellular pathogens.
In addition, EV-035 dramatically increased survival rates in preclinical melioidosis models. This disease is endemic in large parts of Asia and is also seen as a possible bio-terrorist threat by the US Department of Defense, which supported some of the studies on EV-035.
Neil Goldsmith, CEO of Evolva commented, “Rising bacterial resistance and bio-terrorist threats pose pressing challenges. The data Evolva has presented at ICAAC today confirm the potential of EV-035 in addressing these challenges. We are thrilled by the fact that leading experts in this field selected EV-035 to be highlighted at this important conference.”
The following posters on EV-035 are displayed at 2012 ICAAC (Session 248: F-2030-F-2033)
- EV-035: Novel 2-pyridone based topoisomerase inhibitors with broad-spectrum activity against MDR pathogens, including quinolone resistance
- EV-035: in vitro ADMET, mouse PK and efficacy in murine infection models of a new orally available class of antibiotics
- EV-035: Synthesis and in vitro antibacterial activity of a new series of 2-pyridone based topoisomerase inhibitors
- EV-035: Potent antibiotic series against biothreat agent Burkholderia pseudomallei
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