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ETS2101 preclinical progress

22 Jan 2008 07:01

e-Therapeutics plc22 January 2008 Press release 22 January 2008 e-Therapeutics plc ("e-Therapeutics" or "the Company") ETS2101 effective in in vitro studies against skin cancer and commences in vivo studies e-Therapeutics plc (AIM: ETX), the systems biology drug discovery company, todayannounces the successful completion of in vitro testing of its drug candidateETS2101 in melanoma (skin cancer), and its progression into in vivo development. Malignant melanoma is the most aggressive skin cancer, responsible for themajority of skin cancer related deaths, estimated to be more than 48,000 a yearworldwide. Despite many years of intensive research, the only effective cure issurgical removal of the primary tumour at an early stage. Current drugtreatments have limited effect and carry significant toxicity and toleranceproblems. e-Therapeutics is developing ETS2101 as a first-line treatment forthis very serious cancer. In vitro testing of the potency of ETS2101 was carried out by the NorthernInstitute for Cancer Research at Newcastle University, which is supported byCancer Research UK. The same group will also be involved in in vivo testing. ETS2101 cytotoxic against all human melanoma cell-lines tested When tested against a variety of established human melanoma cell-lines,including those derived from melanoma metastases in other tissues, ETS2101 wasprofoundly cytotoxic to all the cell-lines tested at concentrations distributedabout a mean of 14 micro Moles per litre. The results wereconcentration-dependent, following a smooth relationship in all testedcell-lines. ETS2101 induced cell death in metastatic melanoma cells rather than merelyslowing growth Disseminated metastatic melanomas are highly resistant to current drugtherapies. However, ETS2101 did not just slow growth in metastasized cells butwas profoundly cytotoxic to these malignant cells, which are the principal causeof the morbidity of the disease. This observed cytotoxic effect in themetastatic cells in other tissue was very similar to that observed in primarymalignant melanoma cells. This property of ETS2101 is highly desirable as theability to kill distributed melanoma cells, after metastasis has taken place, isa necessary property for a first-line treatment for this type of aggressivecancer. A novel cytotoxic agent with a potentially high therapeutic index The concentrations at which ETS2101 exerts its anti-tumour effects in vitro arecomparable to the plasma levels of ETS2101 that have already been shown to besafe and well-tolerated in several hundred patients. Thus, the cytotoxic actionof ETS2101 appears to be highly selective, leaving normal cells and tissueslargely unaffected, potentially yielding a drug with a high therapeutic index(where the effective dose is only a fraction of that which producesside-effects). Rapid, concentration-dependent killing Cell death in primary malignant and metastatic melanoma cells was as profoundafter exposure for one hour as when exposed for 24 hours, and for five days.Professor Herbie Newell, Professor of Cancer Therapeutics and Director ofScientific Research at the Northern Institute for Cancer Research, who oversawthe testing, said "The observation we have made is that the compound producesconcentration-dependent, but time-independent, effects on cells. This is veryunusual for a cancer drug, where in most cases the effects are time-dependent orconcentration-times-time dependent." ETS2101 is therefore potentially capable ofyielding its effects from a short, perhaps outpatient, treatment visit. Thiswould be an important advantage over existing chemotherapy agents, whichnormally involve sustained high dosing over a long period, with related toxicand very unpleasant side effects. Other cancers targeted by the same compound The cellular mechanisms targeted by ETS2101 are also present in other cancers.e-Therapeutics will seek to demonstrate comparable efficacy in these othercancers, which include breast, colon, ovarian, lymphoma and pancreatic cancers.Since the low toxicity of this molecule has already been demonstrated,e-Therapeutics believes that ETS2101 has high potential as a broad spectrum drugin cancer. Dr Roy Drucker, Medical Director of e-Therapeutics, said: "We are very excitedby the prospects for this compound, not only in melanoma, a very aggressive skincancer, but also in several other serious cancers. In my experience, it is veryunusual to see rapid and complete killing of metastatic cancer cells at aconcentration that suggests such a low side-effect burden for the patient. Ifthese promising results are borne out in the clinic, ETS2101 could become thefuture chemotherapeutic of choice in melanoma." Professor Malcolm Young, the e-Therapeutics CEO, added: "We have now started invivo testing of this exciting candidate. For me, this is drug discovery at itsmost rewarding: ETS2101 showing efficacy in a disease that has been so difficultto address by conventional means shows the power of our systems biology platformto identify promising new treatments, even in the toughest areas." - 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.comAndrew 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.comStephanie Cuthbert Tel: +44 (0) 7843 080 947stephanie.cuthbert@abchurch-group.comAshley Tappashley.tapp@abchurch-group.com Tel: +44 (0) 7944 570 387 About e-Therapeutics 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 candidatetherapies targeted at atherosclerosis, asthma and depression. The Company iscurrently in negotiation with a number of pharmaceutical companies, and isprogressing the preclinical and clinical development of these products. For further information on e-Therapeutics visit www.etherapeutics.co.uk. About in vitro and in vivo testing In vitro testing involves testing of drug candidates in a laboratory medium,such as a cell culture. By contrast, in vivo testing involves testing within aliving organism. This information is provided by RNS The company news service from the London Stock Exchange
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