ETS2101 preclinical progress

e-Therapeutics plc
22 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, today
announces the successful completion of in vitro testing of its drug candidate
ETS2101 in melanoma (skin cancer), and its progression into in vivo development.


Malignant melanoma is the most aggressive skin cancer, responsible for the
majority of skin cancer related deaths, estimated to be more than 48,000 a year
worldwide. Despite many years of intensive research, the only effective cure is
surgical removal of the primary tumour at an early stage. Current drug
treatments have limited effect and carry significant toxicity and tolerance
problems. e-Therapeutics is developing ETS2101 as a first-line treatment for
this very serious cancer.


In vitro testing of the potency of ETS2101 was carried out by the Northern
Institute for Cancer Research at Newcastle University, which is supported by
Cancer 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 was
profoundly cytotoxic to all the cell-lines tested at concentrations distributed
about a mean of 14 micro Moles per litre. The results were
concentration-dependent, following a smooth relationship in all tested
cell-lines.


ETS2101 induced cell death in metastatic melanoma cells rather than merely
slowing growth


Disseminated metastatic melanomas are highly resistant to current drug
therapies. However, ETS2101 did not just slow growth in metastasized cells but
was profoundly cytotoxic to these malignant cells, which are the principal cause
of the morbidity of the disease. This observed cytotoxic effect in the
metastatic cells in other tissue was very similar to that observed in primary
malignant melanoma cells. This property of ETS2101 is highly desirable as the
ability to kill distributed melanoma cells, after metastasis has taken place, is
a necessary property for a first-line treatment for this type of aggressive
cancer.


A novel cytotoxic agent with a potentially high therapeutic index


The concentrations at which ETS2101 exerts its anti-tumour effects in vitro are
comparable to the plasma levels of ETS2101 that have already been shown to be
safe and well-tolerated in several hundred patients. Thus, the cytotoxic action
of ETS2101 appears to be highly selective, leaving normal cells and tissues
largely unaffected, potentially yielding a drug with a high therapeutic index
(where the effective dose is only a fraction of that which produces
side-effects).


Rapid, concentration-dependent killing


Cell death in primary malignant and metastatic melanoma cells was as profound
after exposure for one hour as when exposed for 24 hours, and for five days.
Professor Herbie Newell, Professor of Cancer Therapeutics and Director of
Scientific Research at the Northern Institute for Cancer Research, who oversaw
the testing, said 'The observation we have made is that the compound produces
concentration-dependent, but time-independent, effects on cells. This is very
unusual for a cancer drug, where in most cases the effects are time-dependent or
concentration-times-time dependent.' ETS2101 is therefore potentially capable of
yielding its effects from a short, perhaps outpatient, treatment visit. This
would be an important advantage over existing chemotherapy agents, which
normally involve sustained high dosing over a long period, with related toxic
and 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 other
cancers, 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 drug
in cancer.


Dr Roy Drucker, Medical Director of e-Therapeutics, said: 'We are very excited
by the prospects for this compound, not only in melanoma, a very aggressive skin
cancer, but also in several other serious cancers. In my experience, it is very
unusual to see rapid and complete killing of metastatic cancer cells at a
concentration that suggests such a low side-effect burden for the patient. If
these promising results are borne out in the clinic, ETS2101 could become the
future chemotherapeutic of choice in melanoma.'


Professor Malcolm Young, the e-Therapeutics CEO, added: 'We have now started in
vivo testing of this exciting candidate. For me, this is drug discovery at its
most rewarding: ETS2101 showing efficacy in a disease that has been so difficult
to address by conventional means shows the power of our systems biology platform
to identify promising new treatments, even in the toughest areas.'



                                    - ends -

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About e-Therapeutics

e-Therapeutics plc is a systems biology drug discovery company. It has developed
proprietary computational systems to swiftly and accurately analyse and predict
how medicines interact with cells in the body. This optimises the probability of
identifying drug candidates with desirable efficacy and low toxicity. The
Company 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 novel
antibiotics that have been shown to kill the 'superbug' MRSA, and candidate
therapies targeted at atherosclerosis, asthma and depression. The Company is
currently in negotiation with a number of pharmaceutical companies, and is
progressing 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 a
living organism.






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