Arpida adds novel antibiotic AR-2474 to its preclinical pipeline
In vitro microbiology and proof of concept in topical models of infection
REINACH / BASEL, Switzerland, 8 March 2007 - Arpida Ltd. (SWX: ARPN) today announced positive results of in vitro microbiological studies with AR-2474 against a large panel of clinical isolates, including those resistant to various current therapies. In addition, topical applications of AR-2474 were found to be highly effective in eradicating methicillin resistant Staphylococcus aureus (MRSA) in preclinical models of skin infection and nasal carriage. AR-2474 is a novel antibiotic that is not affected by mechanisms of resistance to other antibiotics, e.g. mupirocin, fusidic acid, erythromycin and clindamycin.
The microbiological studies investigated the activity of AR-2474
against a panel of bacteria known to cause topical infections,
e.g., skin, eye etc. The study was performed on 100 clinical
isolates with various resistance patterns. The panel included 21
MRSA, 27 coagulase-negative staphylococci (CNS), 24 group A
streptococci (GAS) and 28 pneumococci. The compound exhibited
potent activity against all of the isolates and this activity was
unaffected by any pre-existing mechanism of resistance.
Additionally, AR-2474 has been shown to be bactericidal and exhibit
little or no propensity for the development of resistance. The
antibacterial activity and potency of AR-2474 was also confirmed in
vivo against topical gold standard mupirocin (Bactroban®) in
two distinct preclinical models of MRSA infection of the skin and
MRSA nasal carriage. In both models, a preliminary topical
formulation of AR-2474 was at least as efficacious as mupirocin.
Dr. Sergio Lociuro, Head of Research at Arpida Ltd. commented,
"AR-2474 originates from our own research discovery programs and
has now progressed to an advanced pre-clinical stage of
development. We aim to develop AR-2474 as a topical therapy for
different indications including the prevention of MRSA
transmission. In recent years, topical antibiotics like mupirocin
have been extensively used in the healthcare setting to limit the
transmission of MRSA. MRSA and other microbes have become
increasingly resistant to many topical antibiotics, thus
representing a significant emerging clinical issue that requires to
be addressed with novel therapies."
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For further information please contact: Arpida Dr Khalid Islam,
President and CEO Harry Tel: + 41 61 417 96 Welten, MBA, CFO and
Senior Vice President Paul 60 Tel: + 41 61 417 96 Verbraeken, Head
of Corporate Communications 65 Tel: + 41 61 417 96 83
About Arpida Ltd.
Arpida (SWX: ARPN) is a biopharmaceutical company with research
facilities near Basel, Switzerland and in the USA. It focuses on
the discovery and development of novel antibiotic drugs that seek
to overcome the growing problem of bacterial resistance. Arpida's
leading product candidate is intravenous iclaprim, a broad-spectrum
antibiotic that targets severe infections requiring hospital
treatment, including those caused by methicillin-resistant
Staphylococcus aureus (MRSA). In November 2006, intravenous
iclaprim has successfully completed its first Phase III trial in
the treatment of cSSSI (complicated skin and skin structure
infections). The US Food and Drug Administration has granted fast
track status to intravenous iclaprim for the treatment of cSSSI. An
oral formulation of iclaprim has successfully completed three Phase
I trials: a radiolabelled ADME study (absorption, distribution,
metabolism and excretion), a Phase I bioavailability trial with a
solution and one with a capsule formulation. Arpida believes that
the availability of an oral formulation could potentially fulfil an
important clinical medical need for the treatment of serious
bacterial infections, particularly those caused by MRSA. Iclaprim
could be offered not only as an intravenous therapy for hospital
use in acute situations, but also as an oral formulation, allowing
early patient discharge and outpatient treatment.
This switch should be a valuable instrument in reducing healthcare
costs and enhancing patient comfort. Arpida's third most advanced
programme, AR-709, targets upper and lower respiratory tract
infections acquired in the community setting. AR-709 exhibited
potent activity against 611 pneumococcal clinical isolates from
Europe, the USA and Asia irrespective of the mechanisms of
resistance to currently used drugs. Arpida received authorisation
to enter first-in-man studies with AR-709 in the UK in the second
half of 2006. An additional compound, AR-2474, has achieved in vivo
proof of concept. AR-2474 has been shown to be highly effective in
eradicating MRSA in preclinical models of skin infection and nasal
carriage. Moreover, the company has several other leads in
optimisation and additional discovery programmes derived from its
own discovery platform at various research stages. This press
release contains specific forward-looking statements, e.g.
statements including terms like believe, assume, expect or similar
expressions. Such forward-looking statements are subject to known
and unknown risks, uncertainties and other factors which may result
in a substantial divergence between the actual results, financial
situation, development or performance of the company and those
explicitly or implicitly presumed in these statements. Against the
background of these uncertainties readers should not place undue
reliance on forward-looking statements. The company assumes no
responsibility to update forward-looking statements or to adapt
them to future events or developments.
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