New data on three compounds from Basilea’s anti-infectives portfolio presented at ICAAC

Basel, Switzerland - Data on the novel antibiotic compound BAL30072, on ceftobiprole and isavuconazole were presented at the 50th annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in Boston. The data on BAL30072 specifically demonstrate the high in-vitro activity of the new monosulfactam antibiotic against multi-resistant Gram-negative bacteria and elucidate structural elements involved in its unique antimicrobial activity.

Multi-resistant Gram-negative bacteria are appearing with increasing frequency in hospitals around the world causing an increase in mortality, particularly when initial antibiotic therapy does not provide coverage of the causative pathogen, and putting a significant economic burden on healthcare systems. The local emergence of new antibiotic resistance mechanisms against almost all available therapeutics will spread to a worldwide public health problem unless new antibiotics active against multi-resistant bacteria are developed.


BAL30072 - a Trojan horse fighting resistance of Gram-negative bacteria

BAL30072 is a novel siderophore monosulfactam antibiotic that can act like a “Trojan horse” by exploiting natural nutrient uptake systems to gain access to its target. New in-vitro data reveal that a specific structural element of the BAL30072 molecule, the siderophore side chain, contributes directly to its antibacterial activity against clinically increasingly problematic multi-resistant Gram-negative bacteria such as Pseudomonas spp. and Klebsiella spp. (Poster F1‑2132). Furthermore, there is new evidence that an accelerated uptake of BAL30072, facilitated by the compound’s siderophore side chain, potentiates its in-vitro activity against Acinetobacter baumannii, a pathogen which can cause severe pneumonia and infections of the urinary tract and bloodstream (Poster F1-2133).
Basilea is preparing for moving BAL30072 into phase I clinical testing in Q4 2010.

Posters on BAL30072 at ICAAC 2010

The Role of the Siderophore Moiety in the Activity of the Novel Monosulfactam BAL30072. - M. G. P. PAGE, F. RICHALET, C. MÜLLER, B. HOFER, E. DESARBRE; F1-2132

Enhanced Activity of the Siderophore Monosulfactam BAL30072 (BAL) against Acinetobacter in Iron-Limited Conditions. - M. G. PAGE, C. MÜLLER, B. HOFER, E. DESARBRE; F1-2133

Exploring Novel Inhibitors of FOX-4 Class C β-Lactamase. - S. MALLO, C. BETHEL, F. PEREZ-LLARENA, F. PRATI, E. CASELLI, M. PAGE, G. BOU, R. BONOMO; F1-2134

CMY-33, A Novel Extended Spectrum Beta-Lactamase (ESBL) of the CMY-2 Family. - M. TARACILA, A. ENDIMIANI, C. R. BETHEL, Y. DOI, M. G. P. PAGE, R. A. BONOMO; C1-1961

For further information please visit www.icaac.org



Ceftobiprole and isavuconazole - broad-spectrum antimicrobial activity for the treatment of potentially life-threatening infections

A series of posters further adds to the wealth of existing in-vitro and clinical data underscoring the broad-spectrum activity of the antibiotic ceftobiprole against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative pathogens, including Pseudomonas spp. In particular, ceftobiprole demonstrates bactericidal in-vitro activity against clinical isolates of Enterococcus faecalis, unlike other cephalosporins (Poster A1-1376). Enterococci belong to the most common pathogens involved in hospital-associated infections and frequently cause bloodstream infections and wound infections in hospitalized patients. Furthermore, Kim and co-workers unveil in abstract E‑2043 in-vitro results from the Asian Network for Surveillance of Resistant Pathogens (ANSORP) study comprising major respiratory isolates from hospital-acquired pneumonia (HAP) from 10 Asian countries. The authors conclude that ceftobiprole could be an important therapeutic option for HAP caused by resistant pathogens.
Isavuconazole, a novel broad-spectrum triazole in phase III clinical testing against potentially life-threatening invasive fungal infections, showed potent in-vitro activity against a large panel of recent clinical isolates of Aspergillus spp. (Poster M-375).

Posters on ceftobiprole at ICAAC 2010

Pharmacodynamic (PD) Activity of Ceftobiprole (Cefto) Compared to Vancomycin (Vanco) vs. Enterococcus faecalis Using an In Vitro Model. - G. G. ZHANEL, N. LAING, L. COX, E. ROSSNAGEL, D. VOTH, J. A. KARLOWSKY, D. J. HOBAN; A1-1376

Efficacy of Ceftobiprole (BPR) Alone and in Combination with Vancomycin (VAN) in a Rat MRSA Infective Endocarditis (IE) Model. - J. FERNANDEZ, D. ABBANAT, R. K. FLAMM, J. HASTINGS, A. M. BARRON, A. S. LYNCH; B-061

In Vivo Synergism of Ceftobiprole in Combination with Vancomycin against Experimental Endocarditis Due to Vancomycin-Intermediate Staphylococcus aureus. - J. VOUILLAMOZ, J. M. ENTENZA, T. R. VELOSO, M. GIDDEY, P. MOREILLON; B-062

Characterization of β-Lactamase Negative Ampicillin-Resistant (BLNAR) and β-Lactamase Positive Amoxicillin-Clavulanate-Resistant (BLPACR) Haemophilus influenzae. - T. A. DAVIES, A. E. STEVENSON, W. HE, G. J. NOEL, S. I. PELTON; C2-117

In Vitro Activities of Ceftaroline and Ceftobiprole against Penicillin- and Macrolide-Non-Susceptible Streptococcus pneumoniae (SPN)-CANWARD 2009. - A. K. WIERZBOWSKI1, H. J. ADAM, J. KARLOWSKY, D. J. HOBAN, G. G. ZHANEL; E-818

Effects of Ceftobiprole and Comparators Alone and in Combination in an in vitro Staphylococcal Biofilm Model. - D. ABBANAT, C. SANTORO, W. SHANG, E. BAUM, S. CRESPO-CARBONE, A. S. LYNCH; E-1562

In Vitro Activities of Ceftobiprole and Doripenem against Major Bacterial Isolates of Hospital-Acquired Pneumonia in Asian Countries: An ANSORP Study. - S. KIM, J. SONG, D. CHUNG, M. LEE, K. KO, Ansorp Study Group; E-2043

Poster on isavuconazole at ICAAC 2010

Isavuconazole Wild-Type (WT) MIC Distributions and Epidemiological Cut-Off Values (ECVs) for Clinical Isolates of Aspergillus spp. - T. PELÁEZ, A. ESPINEL-INGROFF, B. GAMA, E. REIGADAS, J. GUINEA, L. ALCALÁ, P. MUÑOZ, E. BOUZA; M-375

For further information please visit www.icaac.org



About Basilea

Basilea Pharmaceutica Ltd. is headquartered in Basel, Switzerland, and listed on the SIX Swiss Exchange (SIX:BSLN). Its fully integrated research and development operations are currently focused on antibiotics, antifungals and oncology drugs, as well as on the development of dermatology drugs, targeting the medical challenge of resistance and non-response to current treatment options in the hospital and specialty care setting.
Basilea is currently marketing Toctino® (alitretinoin), the only approved treatment for severe chronic hand eczema unresponsive to potent topical corticosteroids, in Denmark, France, Germany, Switzerland and the United Kingdom and has appointed distributors for Toctino® in other selected European markets, Canada and Mexico. Furthermore, a phase III clinical program on alitretinoin for the treatment of severe chronic hand eczema is ongoing in the U.S. The company has entered into a global partnership with Astellas Pharma Inc. for its phase III compound isavuconazole, a potential best-in-class azole antifungal, for the treatment of life-threatening invasive fungal infections. Full rights to ceftobiprole for the treatment of potentially life-threatening resistant bacterial infections are being transferred back to Basilea from Cilag GmbH International, a Johnson & Johnson company.


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