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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
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