10 Dec 2007 11:18
e-Therapeutics plc10 December 2007 For Immediate Release 10 December 2007 e-Therapeutics plc ("e-Therapeutics" or "the Company") Successful completion of preclinical efficacy and resistance studies of candidate antibiotic ETX1153 against MRSA e-Therapeutics plc (AIM: ETX), the systems biology drug discovery company, ispleased to announce the successful completion of preclinical studies of efficacyand rates of resistance of its candidate antibacterial drug compound ETX1153against methicillin-resistant Staphylococcus aureus (MRSA), commonly referred toin lay terms as one of the hospital "superbugs". High potency ETX1153 has been tested in vitro against numerous strains of MRSA, including thevancomycin intermediately sensitive (VISA) and vancomycin resistant strains(VRSA). ETX1153 was found to be highly potent, with a Minimum InhibitoryConcentration (MIC) below 0.25 microgram/ml for all but three strains tested,for which the median MIC was 0.5 microgram/ml. The most common epidemic strainof MRSA in the UK is EMRSA-16, and this was among the strains killed mosteffectively at the lowest concentration. Furthermore the potency of ETX1153 wascompared with that of other antibiotics commonly used against MRSA, such asmoxifloxacin, trovafloxacin, ciprofloxacin, quinupristin/dalfopristin,linezolid, teichoplanin and vancomycin, and determined to be significantlygreater, showing the lowest MICs among these drugs. Low rate of resistance emergence Initial laboratory studies conducted by e-Therapeutics in 2006 suggested thatthe rate of resistance development of bacteria to ETX1153 was very much lowerthan that to vancomycin. Quantitative comparative studies of the rate ofresistance development, comparing ETX1153 with two antibiotics frequentlyprescribed for MRSA, mupirocin and ciprofloxacin, have confirmed this low rateof resistance. In a study involving 10 common strains of MRSA and awidely-accepted industry model for inducing bacterial resistance, resistantmutants emerged in all the samples for mupirocin and ciprofloxacin, but for 4out of 10 samples for ETX1153 no resistant mutants were observed whatsoever.Across the other samples, the rate of development of resistance to ETX1153 wasorders of magnitude slower than for these frequently prescribed antibiotics. Professor Malcolm Young, Chief Executive of e-Therapeutics commented: "We are delighted that these rigorous studies have confirmed our initial beliefthat ETX1153 could become an important weapon in the battle against thisdevastating bacterial infection. We will aim to progress to clinical studieswith ETX1153 as quickly as possible." - ends - For further information: e-Therapeutics plc www.etherapeutics.co.ukMalcolm Young +44 (0)191 233 1317malcolm@etherapeutics.co.uk Nominated Adviser:WH IrelandRichard Lindley +44 (0)113 394 6628richard.lindley@wh-ireland.co.uk Broker:Cornhill Asset ManagementTom Whitehead +44 (0) 207 645 8327tomw@cornhillassetmanagement.com Andrew Houchin +44 (0) 207 743 6468andrewh@cornhillassetmanagement.com Media enquiries:Abchurch www.abchurch-group.comHeather Salmond Tel: +44 (0) 20 7398 7704heather.salmond@abchurch-group.com Stephanie Cuthbert Tel: +44 (0) 7843 080 947stephanie.cuthbert@abchurch-group.com Ashley Tapp Tel: +44 (0) 7944 570 387ashley.tapp@abchurch-group.com Notes to Editors e-Therapeutics plc is a systems biology drug discovery company. It has developedproprietary computational systems to swiftly and accurately analyse and predicthow medicines interact with cells in the body. This optimises the probability ofidentifying drug candidates with desirable efficacy and low toxicity. TheCompany applies its novel, systematic approach to three areas of activity: • discovery of new drugs; • discovering novel uses for existing drugs; and • analysis of the interactions between different drugs. Amongst e-Therapeutics' pipeline of compounds in development are novelantibiotics that have been shown to kill the "superbug" MRSA, and a novel cancerchemotherapy that has been shown to kill malignant cells at safe doses in a veryshort time. Other candidate therapies in development are targeted atatherosclerosis, asthma and depression. The Company is currently in negotiationwith a number of pharmaceutical companies, and is progressing the preclinicaland clinical development of these products. For further information one-Therapeutics visit www.etherapeutics.co.uk. About MRSA Every year an estimated 100,000 UK patients contract an antibiotic-resistantinfection while in hospital. Cases of MRSA in England and Wales have increasedby 600% in the last decade. The reported cost to the NHS of treating theseinfections is already believed to exceed £1 billion a year. With the steepincrease in the appearance of so-called "super-bugs" such as MRSA in UKhospitals, there is a widely-recognised need for new anti-bacterial treatments. The majority of strains of MSRA are resistant to a wide range of antibiotics andcertain strains are even beginning to exhibit resistance to some of the mostrecently introduced antibiotics such as vancomycin. Minimum inhibitory concentration (MIC) In microbiology, the MIC is the lowest concentration of an antimicrobial thatwill inhibit the visible growth of a microorganism after overnight incubation.The MIC is the routine measure used to quantify the activity of newantimicrobial agents and to identify and monitor resistance of microorganisms toantimicrobial agents. 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